New Articles


Chapter 1. Introduction

Chapter 2. Background

Chapter 3. Linkers for Combinatorial Synthesis

3.1. Resin Derivatization

3.1.1. Convenient Method for Preparing Polystyrene Having beta-Hydroxy Group: Its Application to the Synthesis of Polyethylene Glycol-Grafted Polystyrene Resin Park, B.; Lee, H.; Ryoo, S.; Lee, Y. Tetrahedron Lett. 1997, 38, 591-594.

3.1.2. Solid-Phase Dendrimer Synthesis and the Generation of Super-High_Loading Resin Beads for Combinatorial Chemistry Swali, V.; Wells, N. J.; Langley, G. J.; Bradley, M. J. Org. Chem. 1997, 62, 4902-4903.

3.1.3. Molecular Diversity of Novel Amino Acid Based Dendrimers Mulders, S. J. E.; Brouwer, A. J.; Liskamp, R. M. J. Tetrahedron Lett. 1997, 38, 3085-3088.

3.1.4. Functional Polymers from (Vinyl)polystyrene. Short Routes to Binding Functional Groups to Polystyrene Resin through a Dimethylene Spacer: Bromine, Sulfur, Phosphorus, Silicon, Hydrogen, Boron, and Oxygen Stranix, B. R.; Gao, J. P.; Barghi, R.; Salha, J.; Darling, G. D. J. Org. Chem. 1997, 62, 8987-8993.

3.1.5. Efficient Synthesis of Bromoacetylated Wang Resin Nouvet, A.; Lamaty, F.; Lazaro, R. Tetrahedron Lett. 1998, 39, 3469-3470.

3.1.6. A Reinvestigation of the Preparation, Properties, and Applications of Aminomethyl and 4-Methylbenzhydrylamine Polystyrene Resins Adams, J. H.; Cook, R. M.; Hudson, D.; Jammalamadaka, V.; Lyttle, M. H.; Songster, M. F. J. Org. Chem. 1998, 63, 3706-3716.

3.1.7. PEGA Supports for Combinatorial Peptide Synthesis and Solid-Phase Enzymatic Library Assays Renil, M.; Ferreras, M.; Delaisse, J. M.; Foged, N. T.; Meldal, M. J. Peptide Sci. 1998, 4, 195-210.

3.1.8. Polymer Backbone Disassembly: Polymerisable Templates and Vanishing Supports in High Loading Parallel Synthesis Ball, C. P.; Barrett, A. G. M.; Poitout, L. F.; Smith, M. L.; Thorn, Z. E. Chem. Comm. 1998, 2453-2454.

3.1.9. Preparation, Structure and Morphology of Polymer Supports Sherrington, D. C. Chem. Comm. 1998, 2275-2286.

3.1.10. Soluble Supports Tailored for Organic Synthesis: Parallel Polymer Synthesis via Sequential Normal/Living Free Radical Processes Gravert, D. J.; Datta, A.; Wentworth, P.; Janda, K. D. J. Am. Chem. Soc. 1998, 120, 9481-9495.

3.1.11. A Measure of Solvent Effects on Swelling of Resins for Solid Phase Organic Synthesis Santini, R.; Griffith, M. C.; Qi, M. Tetrahedron Lett. 1998, 39, 8951-8954.

3.1.12. Cleavage and Analysis of Material from Single Resin Beads Wells, N. J.; Davies, M.; Bradley, M. J. Org. Chem. 1998, 63, 6430-6431.

3.1.13. Polymeric Supports for Solid Phase Synthesis Labadie, J. W. Curr. Opin. Chem. Biol. 1998, 2, 346-352.

3.1.14. Polystyrene Grafted Fluoropolymer MicroTubes: New Supports for Solid-Phase Organic Synthesis with Useful Performance at High Temperature Zhao, C.; Shi, S.; Mir, D.; Hurst, D.; Li, R.; Xiao, X. Lillig, J.; Czarnik, A. W. J. Combinatorial Chemistry 1999, 1, 1, 91-95.

3.1.15. On the Development of New Poly(styrene-oxyethylene) Graft Copolymer Resin Supports for Solid-Phase Organic Synthesis Gooding, O. W.; Baudart, S.; Deegan, T. L.; Heisler, K.; Labadie, J. W.; Newcomb, W. S.; Porco, J. A.; van Eikeren, P. J. Combinatorial Chemistry 1999, 1, 1, 113-122.

3.1.16. New high loading paramagnetic support for solid phase organic chemistry Sucholeiki, I.; Perez, J. M.Tetrahedron Lett. 1999,40(18), 3531-3534.

3.1.17. Resin-bound dendrimers as high loading supports for solid phase chemistry A. Mahajan, S. R. Chhabra, W. C. Chan, Tetrahedron Lett. 1999, 40(26), 4909-4912.

3.1.18. Matrix Assisted Synthetic Transformations:  A Mosaic of Diverse Contributions.  I.  The Pattern Emerges Hudson, D.; J. Combinatorial Chemistry 1999, 1, 5, 333-360.

3.1.19. SPOCC: A Resin for Solid-Phase Organic Chemistry and Enzymatic Reactions on Solid Phase Rademann, J., Grotli, M., Meldal, M., Bock, K. J. Am. Chem. Soc.; 1999; 121(23); 5459-5466.

3.1.20. Polymer discs - an alternative support format for solid phase synthesis N. Hird, I. Hughes, D. Hunter, M. G. J. T. Morrison, D. C. Sherrington, L. Stevenson Tetrahedron 1999, 55(31), 9575-9584.

3.1.21. New supports for solid-phase organic synthesis: development of polystyrene resins containing tetrahydrofuran derived cross-linkers P. H. Toy, K. D. Janda Tetrahedron Lett. 1999, 40(35), 6329-6332.

3.1.22. Functional polymers from (vinyl)polystyrene: Recyclable polymer-supported organosilicon protecting groups for solid-phase synthesis Stranix, B.R., Liu, H.Q., & Darling, G.D. J. Org. Chem. 1997, 62, 6183-6186.

3.1.23. A simple method for the generation of chloromethyl polystyrene on the Multipin™ solid support Bui, C. T.; Maeji, N. J.; Rasoul, F.; Bray, A. M. Tetrahedron Lett. 1999, 40(29), 5383 -5386.
 
 

3.2. Linkers for Carboxylic Acids

3.2.1. Calcium-Promoted Hydrolysis of N-Acylureas Allows Mild Release of Peptides Anchored with the Dpr(Phoc) Linker to Hydrophilic Resins Pascal, R.; Sola, R. Tetrahedron Lett. 1997, 38, 4549-4552.

3.2.2. Model Studies for New o-Nitrobenzyl Photolabile Linkers: Substituent Effects on the Rates of Photochemical Cleavage Holmes, C. P. J. Org. Chem. 1997, 62, 2370-2380.

3.2.3. New Fluoride-Labile Linkers for Solid-Phase Organic Synthesis Routledge, A.; Stock, T.; Flitsch, S. L.; Turner, N. J. Tetrahedron Lett. 1997, 38, 8287-8290.

3.2.4. New Synthesis of SASRIN Resin Katritzky, A. R.; Toader, D.; Watson, K.; Kiely, J. S. Tetrahedron Lett. 1997, 38,7849-7850.

3.2.5. An Improved Synthesis and Selective Coupling of a Hydroxy Based Photolabile Linker for Solid Phase Organic Synthesis Whitehouse, D. L.; Savinov, S. N.; Austin, D. J. Tetrahedron Lett. 1997, 38, 7851-7852.

3.2.6. Facile Solid Phase Synthesis of an Activated Diazo Linker Bhalay, G.; Dunstan, A. R. Tetrahedron Lett. 1998, 39, 7803-7806.

3.2.7. The Use of Trichloroacetamide-activated Resin for Ester Formation Phoon, C. W.; Oliver, S. F.; Abell, C. Tetrahedron Lett. 1998, 39, 7959-7962.

3.2.8. An Alkanesulfonamide "Safety-Catch" Linker for Solid-Phase Synthesis Backes, B. J.; Ellman, J. A. J. Org. Chem. 1999, 64, 7, 2322-2330.

3.2.9. HYCRON, an Allylic Anchor for High-Efficiency Solid Phase Synthesis of Protected Peptides and Glycopeptides O. Seitz, H. Kunz J.Org.Chem. 1997, 62, 813-826.

3.2.10. A Novel Resin Linker for Solid-Phase Peptide Synthesis Which Can Be Cleaved Using Two Sequential Mild Reactions A. Zheng, D. Shan, X. Shi, B. Wang J. Org. Chem. 1999; 64(20), 7459-7466.

3.2.11. The pivaloylglycol anchor group: A new platform for a photolabile linker in solid-phase synthesis Peukert, S., Giese, B. J. Org. Chem. 1998, 63, 9045-9051.

3.3. Linkers for Amides

3.3.1. Preparation of Acid-labile Resins with Halide Linkers and their Utility in Solid Phase Organic Synthesis Ngu, K.; Patel, D. V. Tetrahedron Lett. 1997, 38, 973-976.

3.3.2. 9-Hydroxy-9-(4-carboxyphenyl)xanthene-A New Linker for the Synthesis of Peptide Amides Henkel, B.; Zeng, W.; Bayer, E. Tetrahedron Lett. 1997, 38, 3511-3512.

3.3.3. Use of Halomethyl Resins to Immobilize Amines: An Efficient Method for Synthesis of Sulfonamides and Amides on a Solid Support Raju, B.; Kogan, T. P. Tetrahedron Lett. 1997, 38, 4965-4968.

3.3.4. Secondary Amide-based Linkers for Solid Phase Organic Synthesis Swayze, E. E. Tetrahedron Lett. 1997, 38, 8465-8468.

3.3.5. Solid Phase Synthesis of Sec-Amides and Removal from the Polymeric Support Under Mild Conditions Sarantakis, D.; Bicksler, J. J. Tetrahedron Lett. 1997, 38, 7325-7328.

3.3.6. AMEBA: An Acid Sensitive Aldehyde Resin for Solid Phase Synthesis Fivush, A. M.; Willson, T. M. Tetrahedron Lett. 1997, 38, 7151-7154.

3.3.7. Indole Resin: a Versatile New Support for the Solid-Phase Synthesis of Organic Molecules Estep, K. G.; Neipp, C. E.; Stephens Stramiello, L. M.; Adam, M. D.; Allen, M. P.; Robinson, S.; Roskamp, E. J. J. Org. Chem. 1998, 63, 5300-5301.

3.3.8. An Acid- and Base-Stable o-Nitrobenzyl Photolabile Linker for Solid Phase Organic Synthesis Sternson, S. M.; Schreiber, S. L. Tetrahedron Lett. 1998, 39, 7451-7454.

3.3.9. A Backbone Linker for Boc-Based Peptide Synthesis and On-Resin Cyclization:  Synthesis of Stylostatin 1 Bourne, G. T.; Meutermans, W. D. F.; Alewood, P. F.; McGeary, R. P.; Scanlon, M.; Watson, A. A.; Smythe, M. L. J. Org. Chem. 1999, 64, 3095-3101.

3.3.10. Acetophenone-based linker for solid phase synthesis of secondary amides and sulfonamides on the MultipinTM support C. T. Bui, A. M. Bray, F. Ercole, Y. Pham, F. A. Rasoul, N. J. Maeji, Tetrahedron Lett. 1999,40(17), 3471-3474.

3.3.11. Backbone Amide Linker (BAL) Strategy for Solid-Phase Synthesis of C-Terminal-Modified and Cyclic Peptides  K. J. Jensen, J. Alsina, M. F. Songster, J. Vágner, F. Albericio, G. Barany  J. Am. Chem. Soc. 1998, 120, 5441-5452.

3.3.12. The development of solid phase protocols for a backbone amide linker and its application to the Boc-based assembly of linear peptides G. T. Bourne, W. D. F. Meutermans, M. L. Smythe Tetrahedron Lett., 1999, 40, 7271 -7274.

3.3.13. Six new photolabile linkers for solid phase synthesis. 2. Coupling of various building blocks and photolytic cleavage E. A. Akerblom Mol. Diversity, 1999, 4, 53-69.

3.3.14. Solid-phase synthesis of hydroxamic acid based TNF-a convertase inhibitors Barlaam, B.; Koza, P.; Berriot, J. Tetrahedron, 1999, 55(23), 7221-7232.
 
 

3.4. Linkers for Alcohols and Amines

3.4.1. Active Carbonate Resins for Solid-Phase Synthesis Through the Anchoring of a Hydroxyl Function. Synthesis of Cyclic and Alcohol Peptides Alsina, J.; Chiva, C. Ortiz, M.; Rabanal, F.; Giralt, E.; Albericio, F. Tetrahedron Lett. 1997, 38, 883-886.

3.4.2. Solid-Supported tert-Alkoxycarbonylation Reagents for Anchoring of Amines during Solid Phase Organic Synthesis Hernandez, A. S.; Hodges, J. C. J. Org. Chem. 1997, 62, 3153-3157.

3.4.3. A New Cleavage Strategy for the Solid-Phase Synthesis of Secondary Amines Conti, P.; Demont, D.; Cals, J.; Ottenheijm, H. C. J.; Leysen, D. Tetrahedron Lett. 1997, 38, 2915-2918.

3.4.4. 5-(4'-Chloromethylphenyl)pentylpolystyrene Resin (CMPP resin). A New Linker Resin for Solid-Phase Organic Synthesis Under Lewis Acidic Conditions Kobayashi, S.; Moriwaki, M. Tetrahedron Lett. 1997, 38, 4251-4254.

3.4.5. Non-Acidic Cleavage of Wang-Derived Ethers From Solid Support: Utilization of a Mixed-Bed Scavenger For DDQ Deegan, T. L.; Gooding, O. W.; Baudart, S.; Porco, J. A. Tetrahedron Lett. 1997, 38, 4973-4976.

3.4.6. A Novel Formamidine Linker for Use in Solid-Phase Synthesis Furth, P. S.; Reitman, M. S.; Cook, A. F. Tetrahedron Lett. 1997, 38, 5403-5406.

3.4.7. Synthesis of Tertiary Amines Using a Polystyrene (REM) Resin Brown, A. R.; Rees, D. C.; Rankovic, Z.; Morphy, J. R. J. Am. Chem. Soc. 1997, 119, 3288-3295.

3.4.8. A New o-Nitrobenzyl Photocleavable Linker for Solid Phase Synthesis Rodebaugh, R.; Fraser-Reid, B.; Geysen, H. M. Tetrahedron Lett. 1997, 38, 7653-7656.

3.4.9. Carbamate Linkers as Latent N-Methylamines in Solid Phase Synthesis Ho, C. Y.; Kukla, M. J. Tetrahedron Lett. 1997, 38, 2799-2802.

3.4.10. Reagents for Combinatorial Organic Synthesis: Preparation and Uses of Rink-Chloride Garigipati, R. S. Tetrahedron Lett. 1997, 38, 6807-6810.

3.4.11. A 2-Silylethanol-base Anomeric Linker for Carbohydrates; Transformation into 1-O-Acyl Derivatives Wallberg, A.; Weigelt, D.; Falk, N.; Magnusson, G. Tetrahedron Lett. 1997, 38, 4285-4286.

3.4.12. A Base Labile Handle for Solid Phase Organic Chemistry Garcia-Eschevarria, C. Tetrahedron Lett. 1997, 38, 8933-8934.

3.4.13. Resin-Immobilised Benzyl and Aryl Vinyl Sulfones: New Versatile Traceless Linkers for Solid-Phase Organic Synthesis Kroll, F. E. K.; Morphy, R.; Rees, D.; Gani, D. Tetrahedron Lett. 1997, 38, 8573-8576.

3.4.14. Polymer-Bound p-Alkoxybenzyl Trichloracetimidates: Reagents for the Protection of Alcohols as Benzyl Ethers on Solid-Phase Hanessian, S.; Xie, F. Tetrahedron Lett. 1998, 39, 733-736.

3.4.15. Exploring Functional and Molecular Diversity with Polymer-Bound p-Alkoxybenzyl Ethers-Scope and Applications of Preparatively Useful Organic Reactions Hanessian, S.; Xie, F. Tetrahedron Lett. 1998, 39,737-740.

3.4.16. Facile Solid Phase Synthesis of Octreotide Analogs Using p-Carboxybenzaldehyde as a Novel Linker to Anchor Fmoc-Threoninol to Solid Phase Resins Wu, Y. T.; Hsieh, H. P.; Wu, C. Y.; Yu, H. M.; Chen. S. T.; Wang, K. T. Tetrahedron Lett. 1998, 39, 1783-1784.

3.4.17. Alcoholysis and Carbonyl Hydrosilylation Reactions using a Polymer-Supported Trialkylsilane Hu, Y.; Porco, J. A. Tetrahedron Lett. 1998, 39, 2711-2714.

3.4.18. A Linker for Solid Phase Carbohydrate Synthesis, Permitting the Introduction of Variable Anomeric Functionality in the Release Step Weigelt, D.; Magnusson, G. Tetrahedron Lett. 1998, 39, 2839-2842.

3.4.19. Simple and Efficient Synthesis of 2-Chlorotritylchloride Resin Orosz, G.; Kiss, L. P. Tetrahedron Lett. 1998, 39, 3241-3242.

3.4.20. Versatile Dde-Based Primary Amine Linkers for Solid Phase Synthesis Chhabra, S. R.; Khan, A. N.; Bycroft, B. W. Tetrahedron Lett. 1998, 39, 3585-3588.

3.4.21. A Novel Linker for the Attachment of Alcohols to Solid Support Bohm, G.; et al Tetrahedron Lett. 1998, 39, 3819-3822.

3.4.22. PhFl Acetic Acid: A New Linker for Solid Phase Organic Synthesis Bleicher, K. H.; Wareing, J. R. Tetrahedron Lett. 1998, 39, 4591-4594.

3.4.23. Beneficial Participation of the Polymer: Improvement in Polymer-Supported Oligosaccharide Synthesis Mehta, S.; Whitfield, D. Tetrahedron Lett. 1998, 39, 5907-5910.

3.4.24. p-Benzyloxybenzylamine (BOBA) Resin. A New Polymer-Supported Amine Used in Solid-Phase Organic Synthesis Kobayashi, S.; Aoki, Y. Tetrahedron Lett. 1998, 39, 7345-7348.

3.4.25. Design and Synthesis of Silyl Ether-Based Linker for Solid-Phase Synthesis of Glycopeptides Nakamura, K.; Hanai, N.; Kanno, M.; Kobayashi, A.; Ohnishi, Y.; Ito, Y.; Nakahara, Y. Tetrahedron Letters, 1999,40, 3, 515-518.

3.4.26. A Novel Linking-Protecting Group Strategy for Solid-Phase Organic Chemistry with Configurationally Stable alpha-[N-(Phenylfluorenyl)]amino Carbonyl Compounds: Synthesis of Enantiopure Norephedrines on Solid Support Gosselin, F.; Van Betsbrugge, J.; Hatam, M.; Lubell, W. D. J. Org. Chem. 1999, 64, 2486-2493.

3.4.27. Triazenes as Robust and Simple Linkers for Amines in Solid-Phase Organic
Synthesis. S. Bräse, J. Köbberling, D. Enders, R. Lazny, M. Wang, S. Brandtner, Tetrahedron Lett. 1999, 40(11), 2105-2108.

3.4.28.  A Redox-Sensitive Resin Linker for the Solid Phase Synthesis of C-Terminal Modified Peptides Zheng, A.; Shan, D.; Wang, B. J. Org. Chem. 1999, 64, 156-161.

3.4.29. Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis Schiemann, K.; Showalter, H. D. H. J. Org. Chem. 1999, 64, 4972-4975.

3.4.30.  Preparation of Polymer-Bound 1H-Benzotriazole, a New Potential Scaffold for the Compilation of Organic Molecule Libraries Katritzky, A. R.; Belyakov, S. A.; Tymoshenko, D. O. J. Comb. Chem. 1999, 1, 2, 173-176.

3.4.31. Solid-Supported Benzotriazoles: Synthetic Auxiliaries and Traceless Linkers for the Combinatorial Synthesis of Amine Libraries Paio, A.; Zaramella, A.; Ferritto, R.; Conti, N.; Marchioro, C.; Seneci, P. J. Comb. Chem. 1999, 1, 4, 317-325.

3.4.32. Immobilizations of Nucleophiles on Polystyrene Supports Brill, W. K. D.; Schmidt, E., and Tommasi, R. A.  Synlett 1998; 8, 906-908.

3.4.33. Application of Polymer Supported Base in Solid Phase Synthesis - Convenient Synthesis of N-Aryl-N'-Benzyl Piperazine Derivatives Yamamoto, Y.; Tanabe, K., and Okonogi, T. Chem. Lett. 1999; (2):103-104.

3.4.34. A Cyclitively Cleavable Linker for Alcohols: Linker Preparation and Cleavage Conditions Xiao, X.-Y.; Nova, M. P.; Czarnik, A. W. J. Combinatorial Chemistry 1999, 1, 5, 379-382.

3.4.35. Dihydropyran-2-carboxylic acid, a novel bifunctional linker for the solid-phase synthesis of peptides containing a C-terminal alcohol Hsieh, H-.P., Wu, Y.T., Chen, S.T., & Wang, K.T. Chem. Commun. 1998, 649-650.

3.4.36. Glycosidation of solid-supported glycosyl donors tethered by a trialkylsilane linker Doi, T.; Sugiki, M.; Yamada, H.; Takahashi, T. Tetrahedron Lett. 1999, 40, 2141-2144.

3.4.37. Use of Quinic Acid as Template in Solid-Phase Combinatorial Synthesis Phoon, C. W.; Abell, C. Journal of Combinatorial Chemistry 1999, 1(6), 485-492.

3.5. Linkers for Hydrocarbons and Other Functional Groups

3.5.1. A TFA-Cleavable Linkage for Solid-Phase Synthesis of Hydroxamic Acids Richter, L. S.; Desai, M. C. Tetrahedron Lett. 1997, 38, 321-322.

3.5.2. Germanium and Silicon Linking Strategies for Traceless Solid-Phase Synthesis Plunkett, M. J.; Ellman, J. A. J. Org. Chem. 1997, 62, 2885-2893.

3.5.3. Traceless Linker: Oxidative Activation and Displacement of a Sulfur-Based Linker Suto, M. J.; Gayo, L. M. Tetrahedron Lett. 1997, 38, 211-214.

3.5.4. The Use of a Dithiane Protected Benzoin Photolabile Safety Catch Linker for Solid-Phase Synthesis Routledge, A.; Abell, C.; Balasubramanian, S. Tetrahedron Lett. 1997, 38, 1227-1230.

3.5.5. A Linker for Amidines in Solid Phase Synthesis Roussel, P.; Bradley, M.; Matthews, I.; Kane, P. Tetrahedron Lett. 1997, 38, 4861-4864.

3.5.6. Development of New Linkers for the Formation of Aliphatic C-H Bonds on Polymeric Supports Jung, K. W.; Zhou, X.; Janda, K. D. Tetrahedron Lett. 1997, 53, 6645-6652.

3.5.7. Soluble Polymer Synthesis: An Improved Traceless Linker Methodology for Aliphatic C-H Bond Formation Zhao, X.; Jung, K. W.; Janda, K. D. Tetrahedron Lett. 1997, 38, 977-980.

3.5.8. A Silicon Linker for Direct Loading of Aromatic Compounds to Supports. Traceless Synthesis of Pyridine-Based Tricyclics Woolard, F. X.; Paetsch, J.; Ellman, J. A. J. Org. Chem. 1997, 62, 6102-6103.

3.5.9. A New and Efficient Solid Phase Synthesis of Hydroxamic Acids Ngu, K.; Patel, D. V. J. Org. Chem. 1997, 62, 7088-7089.

3.5.10. A Novel Linkage for the Solid-Phase Synthesis of Hydroxamic Acids Bauer, U.; Ho, W.-B.; Koskinen, A. M. P. Tetrahedron Lett. 1997, 38, 7233-7236.

3.5.11. Facile Prparation of Chloromethylaryl Solid Supports Using Methanesulfonyl Chloride and Hunig's Base Nuigiel, D. A.; Wacker, D. A.; Nemeth, G. A. Tetrahedron Lett. 1997, 38, 5789-5790.

3.5.12. The Use of Thioesters in Solid Phase Organic Synthesis Vlattas, I.; Dellureficio, J.; Dunn, R.; Sytwu, I. I.; Stanton, J. Tetrahedron Lett. 1997, 38, 7321-7324.

3.5.13. A Simple Linker for the Attachment of Aldehydes to the Solid Phase. Application to Solid Phase Synthesis by the Multipin Method Ede, N. J.; Bray, A. M. Tetrahedron Lett. 1997, 38, 7119-7122.

3.5.14. Solid-Phase Synthesis of Arginine-Containing Peptides by Guanidine Attachment to a Sulfonyl Linker Zhong, H. M.; Greco, M. N.; Maryanoff, B. E. J. Org. Chem. 1997, 62, 9326-9330.

3.5.15. Novel Serine-Based Linker for the Solid-Phase Synthesis of Organic Compounds Chou, Y.-L.; Morrissey, M. M.; Mohan, R. Tetrahedron Lett. 1998, 39, 757-760.

3.5.16. A Highly Acid Labile Silicon Linker for Solid Phase Synthesis Hone, N. D.; Davies, S. G.; Devereux, N. J.; Taylor, S. L.; Baxter, A. D. Tetrahedron Lett. 1998, 39, 897-900.

3.5.17. Arylsulfonate Esters in Solid Phase Organic Synthesis. I. Cleavage with Amines, Thiolate, and Imidazole Rueter, J. K.; Nortey, S. O.; Baxter, E. W.; Leo, G. C.; Reitz, A. B. Tetrahedron Lett. 1998, 39, 975-978.

3.5.18. Arylsulfonate Esters in Solid Phase Organic Synthesis. II. Compatibility with Commonly-Used Reaction Conditions Baxter, E. W.; Rueter, J. K.; Nortey, S. O.; Reitz, A. B. Tetrahedron Lett. 1998, 39, 979-982.

3.5.19. Decarboxylation-Based Traceless Linking with Aroyl Acrylic Acids Garibay, P.; Nielsen, J.; Hoeg-Jensen, T. Tetrahedron Lett. 1998, 39, 2207-2210.

3.5.20. Solid Supported Synthesis of Hydroxamic Acids Golebiowski, A.; Klopfenstein, S. Tetrahedron Lett. 1998, 39, 3397-3400.

3.5.21. Novel Phosphate Ester-Linked Resins: The Solid-Phase Generation of Phenyl Phosphate-Containing Compounds for SH2 Inhibition Metcalf, C. A.; Vu, C. B.; Sundaramoorthi, R.; Jacobsen, V. A.; Laborde, E. A.; Green, J.; Green, Y.; Macek, K. J.; Merry, T. J.; Pradeepan, S. G.; Uesugi, M.; Varkhedkar, V. M.; Holt, D. A. Tetrahedron Lett. 1998, 39, 3435-3438.

3.5.22. Reductive Cleavage of Resin Bound Arylsulfonates Jin, S.; Holub, D. P.; Wustrow, D. J. Tetrahedron Lett. 1998, 39, 3651-3654.

3.5.23. Solid Phase Synthesis of Urea Libraries Using a Diversifiable Thiophenoxy Carbonyl Linker Dressman, B. A.; Singh, U.; Kaldor, S. W. Tetrahedron Lett. 1998, 39, 3631-3634.

3.5.24. Novel Polymer-Supported Trialkylsilanes and Their Use in Solid-Phase Organic Synthesis Hu, Y.; Porco, J. A.; Labadie, J. W.; Gooding, O. W.; Trost, B. M. J. Org. Chem. 1998, 63, 4518-4521.

3.5.25. Novel Method for the Loading of Nucleophiles on Multipin Crowns Tommasi, R. A.; Nantermet, P. G.; Shapiro, M. J.; Chin, J.; Brill, W. K.-D.; Ang, K. Tetrahedron Lett. 1998, 39, 5477-5480.

3.5.26. A Practical Method for the Combinatorial Synthesis of Peptide Aldehydes Hall, B. J.; Sutherland, J. D. Tetrahedron Lett. 1998, 39, 6593-6596.

3.5.27. A Facile and Convenient Solid-Phase Procedure for Synthesizing Nucleoside Hydroxamic Acids Khan, S. I.; Grinstaff, M. W. Tetrahedron Lett. 1998, 39, 8031-8034.

3.5.28. Solid-Phase Synthesis of N-Substituted Amidinophenoxy Pyridines as Factor Xa Inhibitors Mohan, R.; Yun, W.; Buckman, B. O.; Liang, A.; Trinh, L.; Morrissey, M. M. Bioorg. Med. Chem. Lett. 1998, 8, 1877-1882.

3.5.29. Novel Polymer-Supported Trialkylsilanes and Their Use in Solid-Phase Organic Synthesis Hu, Y.; Porco, J. A.; Labadie, J. W.; Gooding, O. W. J. Org. Chem. 1998, 63, 4518-4521.

3.5.30. Selenium-Linking Strategy for Traceless Solid-Phase Synthesis:  Direct Loading, Aliphatic C-H Bond Formation Upon Cleavage and Reaction Monitoring by Gradient MAS NMR Spectroscopy Ruhland, T.; Andersen, K.; Pedersen, H. J. Org. Chem. 1998, 63, 9204-9211.

3.5.31. Solid-Phase Synthesis of Peptidyl Trifluoromethyl Ketones Poupart, M.-A.; Fazal, G.; Goulet, S.; Mar, L. T. J. Org. Chem. 1999, 64, 1356-1361.

3.5.32. Parallel Synthesis of Aldehydes and Ketone Facilitated by a New Solid-Phase Weinreb Amide Salvino, J. M.; Mervic, M.; Mason, H. J.; Siesow, T.; Teager, D.; Airey, J.; Labaudiniere, R. J. Org. Chem. 1999, 64, 1823-1830.

3.5.33. A Novel, Thioacetal Based Linker for Solid-Phase Synthesis Huwe, C. M.; Kunzer, H. Tetrahedron Letters, 1999, 40, 4, 683-686.

3.5.34. Chromium carbonyl complexes as novel traceless linkers S. E. Gibson, N. J. Hales, M. A. Peplow, Tetrahedron Lett. 1999,40, 7, 1417-1418.

3.5.35.  Solid-Phase Synthesis of Hydroxamic Acids Dankwardt, S. M.  Synlett 1998; 7, 761-761.

3.5.36. Nucleophilic Substitutions on Multipin(TM) Systems Linked with a Traceless Linker Takahashi, T.; Tomida, S.; Inoue, H., and Doi, T. Synlett 1998; 11, 1261-1263.

3.5.37. Practical Preparation of First Carbon Linked Polymer-Bound 1,3-Diol Chandrasekhar, S.; Padmaja, M. B.  Synth. Commun.1998;28(19):3715-3720.

3.5.38. An Oxidation-Labile Traceless Linker for Solid-Phase Synthesis Stieber, F.; Grether, U.; Waldmann, H. Angew. Chem. Int. Ed. 1999, 38(8), 1073-1077.

3.5.39. Efficient Cleavage-Cross-Coupling Strategy for Solid-Phase Synthesis - A Modular Building System for Combinatorial Chemistry Brase, S.; Schroen, M. Angew. Chem. Int. Ed. 1999, 38(8), 1071-1073.

3.5.40. A Surprising Solid-Phase Effect - Development of a Recyclable Traceless Linker System for Reactions on Solid Support Brase, S.; Enders, D.; Kobberling, J., and Avemaria, F. Angew. Chem. Int. Ed. 1998,37, 24, 3413-3415.

3.5.41. Solid Phase Synthesis of C-Terminal Peptide Aldehydes Fehrentz, J. A.; Paris, M.; Heitz, A.; Velek, J.; Winternitz, F.; Martinez, J. J.Org.Chem. 1997,62, 6792-6796.

3.5.42. A new linker for the synthesis of C-terminal peptide alpha-oxo-aldehydes Fruchart, J.-S.; Gras-Masse, H.; Melnyk, O. Tetrahedron Lett. 1999, 40(34), 6225-6228.

3.5.43. Simple silyl linker for the solid phase organic synthesis of aryl-containing molecules Newlander, K.A.; Chenera, B.; Veber, D.F.; Yim, N.C.; Moore, M.L. J. Org. Chem. 1997, 62, 6726-6732.

3.5.44. Solid-phase synthesis of 2-methoxyaniline derivatives by the traceless silicon linker strategy Curtet, S.; Langlois, M. Tetrahedron Lett. 1999, 40(49), 8563-8566.

 


Chapter 4. Combinatorial Solid Phase Synthesis

4.1. Condensations to Prepare Amides, Esters, Ureas, Imines, Phosphorus, and Other Related Compounds

4.1.1. Solid-Phase Synthesis via N-Terminal Attachment to the 2-Chlorotrityl Resin Hoekstra, W. J.; Greco, M. N.; Yabut, S. C.; Hulshizer, B. L.; Maryanoff, B. E. Tetrahedron Lett. 1997, 38, 2629-2632.

4.1.2 Azido Acids in a Novel Method of Solid-Phase Peptide Synthesis Meldal, M.; Julianok, M. A.; Janson, A. M. Tetrahedron Lett. 1997, 38, 2531-2534.

4.1.3. Solid Phase Synthesis of Ureas of Secondary Amines via Carbamoyl Chloride Wang, G. T.; Chen, Y.; Wang, S.; Sciotti, R.; Sowin, T. Tetrahedron Lett. 1997, 38, 1895-1898.

4.1.4. Solid-Phase Synthesis of Trisubstituted Guanidines Drewry, D. H.; Gerritz, S. W.; Linn, J. A. Tetrahedron Lett. 1997, 38, 3377-3380.

4.1.5. Solid Phase Synthesis of Sulfonamides Using a Carbamate Linker Raju, B.; Kogan, T. P. Tetrahedron Lett. 1997, 38, 19, 3373-3376.

4.1.6. Solid-Phase Synthesis via 5-Oxazolidinones. Ring-Opening Reactions with Amines and Reaction Monitoring by Single-Bead FT-IR Microspectroscopy Marti, R. E.; Yan, B.; Jarosinski, M. A. J. Org. Chem. 1997, 62, 5615-5618.

4.1.7. Solid Phase Synthesis of Substituted Aminosulfonyl Ureas Using a Sulfonylcarbamate Linker Fitzpatrick, L. J.; Rivero, R. A. Tetrahedron Lett. 1997, 38, 7479-7482.

4.1.8. Solid Phase Synthesis of Trisubstituted Guanidines Drewry, D. H.; Gerritz, S. W.; Linn, J. A. Tetrahedron Lett. 1997, 38, 3377-3380.

4.1.9. Solid Phase Synthesis of Cyanoacetamidines: Fast Access to Potential Bioisosteres of Acceptor-Substituted Guanidines Zaragoza, F. Tetrahedron Lett. 1997, 38, 7291-7294.

4.1.10. Solid Phase Synthesis of beta-Peptides via Arndt-Eistert Homologation of Fmoc-Protected Amino Acid Diazoketones Marti, R. E.; Bleicher, K. H.; Bair, K. W. Tetrahedron Lett. 1997, 38, 6145-6148.

4.1.11. Phosphorus-Based Combinatorial Libraries: Use of Amino Acid Derivatives as Synthons Fathi, R.; Patel, R.; Cook, A. F. Molec. Div. 1996, 2, 125-134.

4.1.12. Solid-Phase Synthesis of Disubstituted Guanidines Kearney, P. C.; Fernandez, M.; Flygare, J. A. Tetrahedron Lett. 1998, 39, 2663-2666.

4.1.13. Solid Phase Synthesis of Phosphinopeptoids as Transition State Analog Inhibitors Dorff, P. H.; Chiu, G.; Goldstein, S. W.; Morgan, B. P. Tetrahedron Lett. 1998, 39, 3375-3378.

4.1.14. N-Linked Solid Phase Peptide Synthesis Leger, R.; Yen, R.; She, M. W.; Lee, V. J.; Hecker, S. J. Tetrahedron Lett. 1998, 39,4171-4174.

4.1.15. Solid Phase Synthesis of Combinatorial Libraries Using Anhydrides as Templates Perumattam, J.; Chakravarty, S.; McEnroe, G. A.; Goehring, R. R.; Mavunkel, B.; Suravajjala, S.; Smith, W. W.; Chen, B. Molecular Diversity 1998, 3, 121-128.

4.1.16. Phosgenated p-Nitrophenyl(polystyrene)ketoxime or Phoxime Resin. A New Resin for the Solid-Phase Synthesis of Ureas via Thermolytic Cleavage of Oxime-Carbamates Scialdone, M. A.; Shuey, S. W.; Soper, P.; Hamuro, Y.; Burns, D. M. J. Org. Chem. 1998, 63, 4802-4807.

4.1.17. Preparation of Amides from Acids and Resin Bound Azides:  Suppression of Intramolecular Lactam Formation Tang, Z.; Pelletier, J. C. Tetrahedron Lett. 1998, 39, 4773-4776.

4.1.18. Practical Method for the Parallel Synthesis of 2'-Amido-2'-deoxyadenosines Link, A.; Calenbergh, S. van; Herdewijn, P. Tetrahedron Lett. 1998, 39, 5175-5176.

4.1.19. Solid-Phase Synthesis of N,N' Substituted Guanidines Dodd, D. S.; Wallace, O. B. Tetrahedron Lett. 1998, 39, 5701-5704.

4.1.20. Novel Linker for the Solid-Phase Synthesis of Guanidines Josey, J. A.; Tarlton, C. A.; Payne, C. E. Tetrahedron Lett. 1998, 39, 5899-5902.

4.1.21. Transprotection in Solid Phase Peptide Synthesis:  Easy Conversion of Fmoc Carbamates into Boc Carbamates Furlan, R. L. E.; Mata, E. G. Tetrahedron Lett. 1998, 39, 6421-6422.

4.1.22. Construction of Combinatorial Chemical Libraries Using a Rapid and Efficient Solid Phase Synthesis Based on a Multicomponent Condensation Reaction Kim, S. W.; Bauer, S. M.; Armstrong, R. W. Tetrahedron Lett. 1998, 39, 6993-6996.

4.1.23. Solid and Solution Phase Combinatorial Synthesis of Ureas Nieuwenhuijzen, J. W.; Conti, P. G. M.; Ottenheijm, H. C. J.; Linders, J. T. M. Tetrahedron Lett. 1998, 39, 7811-7814.

4.1.24. Kinetic Comparison of Amide Formation on Various Cross-Linked Polystyrene Resins Li, W.; Xiao, X.; Czarnik, A. W. J. Combinatorial Chemistry 1999, 1, 2, 127-129.

4.1.25. Solid-Phase Synthesis of Acyclic and Cyclic Amino Acid Derived Urea Peptidomimetics Using Phoxime Resin Hamuro, Y.; Marshall, W. J.; Scialdone, M. A. J. Combinatorial Chemistry 1999, 1, 2, 163-172.

4.1.26. A New Reagent for Solid and Solution Phase Synthesis of Protected
Guanidines From Amines Yong, Y. F.; Kowalski, J. A.; Thoen, J. C.; Lipton, M. A.Tetrahedron Lett., 40, 1, 53-56.

4.1.27. A Simple Procedure for the Solid Phase Synthesis of Unsymmetrically Functionalised Diamides from Symmetric Diacids Wahhab, A.; Leban, J. Tetrahedron Lett., 40, 2, 235-238.

4.1.28. Preparation and Use of N-Hydroxysuccinimidyl Active Ester Resins Adamczyk, M.; Fishpaugh, J. R.; Mattingly, P. G. Tetrahedron Lett. 1999, 40, 463-466.

4.1.29. Soluble Polymer-Supported Synthesis of N,N-di(BOC)-Protected Guanidines  Shey, J. Y. and Sun, C. M. Synlett 1998, 12, 1423-1425.

4.1.30. Solid Support-Bound Synthesis of Polyfunctional Unsymmetrical Ureas Maurer, K. W. and Kenyon, G. L.  Bioorg. Chem. 1997;25(5-6):277-281.

4.1.31. Solid phase synthesis of aryl and heteroaryl amines using the Curtius rearrangement S. Sunami, T. Sagara, M. Ohkubo, H. Morishima Hiemstra, Tetrahedron Lett. 1999, 40(9), 1721-1724.

4.1.32. Solid-phase synthesis of N,N'-unsymmetrically substituted ureas: application to the synthesis of carbaza peptides D. Limal, V. Semetey, P. Dalbon, M. Jolivet, J.-P. Briand, Tetrahedron Lett.1999,40(14), 2749-2752.

4.1.33. Microwave-assisted solid-phase Ugi four-component condensations A. M. L. Hoel, J. Nielsen, Tetrahedron Lett. 1999, 40(20), 3941-3944.

4.1.34. A traceless linker approach to the solid phase synthesis of substituted guanidines utilizing a novel acyl isothiocyanate resin L. J. Wilson, S. R. Klopfenstein, M. Li, Tetrahedron Lett. 1999,40(21), 3999-4002.

4.1.35. Solid phase urea synthesis: an efficient and direct conversion of Fmoc-protected amines to ureas P. Y. Chong, P. A. Petillo, Tetrahedron Lett. 1999, 40(24), 4501-4504.

4.1.36.  Novel Solid-Phase Synthesis of Azapeptides and Azapeptoides via Fmoc-Strategy and Its Application in the Synthesis of RGD-Mimetics C. Gibson, S. L. Goodman, D. Hahn, G. Hölzemann, H. Kessler J. Org. Chem. 1999, 64(20), 7388-7394.

4.1.37. Convergent Synthesis of Dolastatin 15 by Solid Phase Coupling of an N-Methylamino Acid Akaji, K., Hayashi, Y., Kiso, Y., Kuriyama, N. J. Org. Chem. 1999, 64(2), 405-411.

4.1.38. Solid phase synthesis of aza peptides using an automatic synthesizer Ahn, I-A, Kim, S. W., Ro S. Mol. Diversity 1999, (4), 23-24.

4.1.39. N-Fmoc-Aminooxy-2-chlorotrityl polystyrene resin: A facile solid-phase methodology for the synthesis of hydroxamic acids Mellor, S.L., McGuire, C., Chan, W.C. Tetrahedron Lett. 1997, 38, 3311-3314.

4.1.40. A novel synthesis of diethyl 1-aminoarylmethylphosphonates on the surface of alumina Sardarian, A.R., & Kaboudin, B. Tetrahedron Lett. 1997, 38, 2543-2546.

4.1.41. Solid-phase synthesis of tri-functionalised, alpha-substituted carbamoylmethyl-homocysteine compounds, their release from the resin and subsequent intramolecular cyclisation to give novel 1,3,3-trisubstituted succinimides Girdwood, J.A., & Shute, R.E. Chem. Commun. 1997, 2307-2308.

4.1.42. Impurity Annihilation - A Strategy for Solution-Phase Combinatorial Chemistry with Minimal Purification Barrett, A. G. M.; Smith, M. L., and Zecri, F. J. Chem. Comm. 1998; 21, 2317-2318.

4.1.43. Solid phase synthesis of guanidines Robinson, S.; Roskamp, E.J. Tetrahedron 1997, 53, 6697-6705.

4.1.44. Automated synthesis and purification of amides: Exploitation of automated solid phase extraction in organic synthesis Lawrence, R.M.; Biller, S.A.; Fryszman, O.M.; Poss, M.A. Synthesis-Stuttgart 1997, 553-558.

4.2. Carbon-Carbon Bond Formation on Solid Support

4.2.1. Solid-Phase Synthesis of Peptide Mimetics with (E)-Alkene Amide Bond Replacements Derived from Alkenylaziridines Wipf, P.; Henninger, T. C. J. Org. Chem. 1997, 62, 1586-1587.

4.2.2. A New Approach to the Solid-Phase Suzuki Coupling Reaction Piettre, S. R.; Baltzer, S. Tetrahedron Lett. 1997, 38, 1197-1200.

4.2.3. Combinatorial Synthesis of C(2), C(3)-Disubstituted 3-Hydroxypropionamides Utilizing Baylis-Hilman Reactions on Solid Support Prien, O.; Rolfing, K.; Thiel, M.; Kunzer, H. Synlett 1997, 3, 325-326.

4.2.4. Solid Phase Synthesis of Ketones from Esters Wallace, O. B. Tetrahedron Lett. 1997, 38, 4939-4942.

4.2.5. The Solid Phase Synthesis of Disubstituted Unnatural Amino Acids and Peptides (di-UPS) Scott, W. L.; Zhou, C.; Fang, Z.; O'Donnell, M. J. Tetrahedron Lett. 1997, 38, 3695-3698.

4.2.6. Solid Phase Synthesis of Unnatural Amino Acids using Unactivated Alkyl Halides O'Donnell, M. J.; Lugar, C. W.; Pottorf, R. S.; Zhou, C.; Scott, W. L.; Cwi, C. L. Tetrahedron Lett. 1997, 38, 3695-3698.

4.2.7. Tandem UPS: Sequential Mono- and Dialkylation of Resin-Bound Glycine via Automated Synthesis Griffith, D. L.; O'Donnell, M. J.; Pottorf, R. S.; Scott, W. L.; Porco, J. A. Tetrahedron Lett. 1997, 38, 8821-8824.

4.2.8. Solid-Phase Synthesis of 4-Arylazetidine-2-ones via Suzuki and Heck Cross-Coupling Reactions Ruhland, B.; Bombrun, A.; Gallop, M. A. J. Org. Chem. 1997, 62, 7820-7826.

4.2.9. Asymmetric Crotylation Reactions on Solid Support: Synthesis of Stereochemically Well-Defined Polypropionate-Like Subunits Panek, J. S.; Zhu, B. J. Am. Chem. Soc. 1997, 119, 12022-12023.

4.2.10. A New Attachment/Cleavage Strategy: Polymer Bound Allylic Sulfones in a Solid-Phase Route to Trisubstituted Olefins Halm, C.; Evarts, J.; Kurth, M. J. Tetrahedron Lett. 1997, 38, 7709-7712.

4.2.11. Solid Phase Heterocyclic Synthesis via Ring Closing Metathesis: Traceless Linking and Cyclative Cleavage Through a Carbon-Carbon Double Bond Piscopio, A. D.; Miller, J. F.; Koch, K. Tetrahedron Lett. 1997, 38, 7143-7146.

4.2.12. Ring Opening Cross-Metathesis on Solid Support Cuny, G. D.; Cao, J.; Hauske, J. R. Tetrahedron Lett. 1997, 38, 5237-5240.

4.2.13. New Multi-Coupling Benzylic Zinc Reagents for the Preparation of Flexible Aromatic Compounds Rottlander, M.; Knochel, P. Tetrahedron Lett. 1997, 38, 1749-1752.

4.2.14. Macrocyclization on Solid Support using Heck Reaction Akaji, K.; Kiso, Y. Tetrahedron Lett. 1997, 38, 5185-5188.

4.2.15. Synthesis of Primary Amines via Nucleophilic Addition of Organicmetallic Reagents to Aldimines on Solid Support Katritzky, A. R.; Xie, L.; Zhang, G.; Griffith, M.; Watson, K.; Kiely, J. S. Tetrahedron Lett. 1997, 38, 7011-7014.

4.2.16. Solid-Phase Synthesis of Novel Amino-Ether Derivatives Furth, P. S.; Reitman, M. S.; Gentles, R.; Cook, A. F. Tetrahedron Lett. 1997, 38, 6643-6646.

4.2.17. Synthesis of Chrial alpha-Substituted beta-Hydroxy Acid Derivatives on Solid Support Purandare, A. V.; Natarajan, S. Tetrahedron Lett. 1997, 38, 8777-8780.

4.2.18. Solid Phase Synthesis of 2-Aminobutadienes Using a Piperazine Linker Hird, N. W.; Irie, K.; Nagai, K. Tetrahedron Lett. 1997, 38, 7111-7114.

4.2.19. Synthesis of 3,4,5-Trisubstituted Cyclohexanones by Cycloaddition to Solid Phase 2-Aminobutadienes Crawshaw, M.; Hird, N. W.; Irie, K.; Nagai, K. Tetrahedron Lett. 1997, 38, 7115-7118.

4.2.20. Transformation of Resin-Bound Pyridinium Ylides: I. A Stereoselective Synthesis of 2,2,3-Trisubstituted Cyclopropanecarboxylates Vo, N. H.; Eyermann, C. J.; Hodge, C. N. Tetrahedron Lett. 1997, 38, 7951-7954.

4.2.21. Intermolecular Free Radical Reactions on Solid Support. Allylation of Esters Sibi, M. P.; Chandramouli, S. V. Tetrahedron Lett. 1997, 38, 8929-8932.

4.2.22. Mannich Reactions of Resin-Bound Substrates: 2. A Versatile Three-Component Solid-Phase Organic Synthesis Methodology McNally, J. J.; Youngman, M. A.; Dax, S. L. Tetrahedron Lett. 1998, 39, 967-970.

4.2.23. Solid-Phase Preparation of Dienes Blaskovich, M. A.; Kahn, M. J. Org. Chem. 1998, 63, 1119-1125.

4.2.24. Solid Phase Synthesis of Macrocycles by an Intramolecular Ketophosphonate Reaction. Synthesis of a (dl)-Muscone Library Nicolaou, K. C.; Pastor, J.; Winssinger, N.; Murphy, F. J. Am. Chem. Soc. 1998, 120, 5132-5133.

4.2.25. Solid Phase Aldol and Conjugate Addition Reactions Using Evans' Oxazolidinone Chiral Auxiliary Phoon, C. W.; Abell, C. Tetrahedron Lett. 1998, 39, 2655-2658.

4.2.26. Solid-Phase Functionalization of Heterocycles by Direct Lithiation Li, Z.; Ganesan, A. Synlett 1998, 405.

4.2.27. Ruthenium-Catalyzed Yne-Ene Cross Metathesis Binding to Solid Support and Cleavage by Pd(0)-Catalysis Schurer, S. C.; Blechert, S. Synlett1998, 166-168.

4.2.28. Ruthenium-Catalyzed Yne-Ene Cross Metathesis Immobilization of Functionalized Alkynes Schuster, M.; Blechert, S. Tetrahedron Lett. 1998, 39, 2295-2298.

4.2.29. Knoevenagel Condensation of Unsymmetrical Malonamic Esters and Malonates on a Solid Support Hamper, B. C.; Kolodziej, S. A.; Scates, A. M. Tetrahedron Lett. 1998, 39, 2047-2050.

4.2.30. Solid-Phase Synthesis of Substituted Glutamic Acid Derivatives via Michael Addition Reactions Dominguez, E.; O'Donnell, M. J.; Scott, W. L. Tetrahedron Lett. 1998, 39, 2167-2170.

4.2.31. Solid-Phase C-Acylation of Active Methylene Compounds Sim, M. M.; Lee, C. L.; Ganesan, A. Tetrahedron Lett. 1998, 39, 2195-2198.

4.2.32. SmI2-Mediated Sequential Radical Cyclization/Anionic Capture of Aryl Iodides on Solid Support Du, X.; Armstrong, R. W. Tetrahedron Lett. 1998, 39, 2281-2284.

4.2.33. Substituted Sulfonamides via a Three Component Reaction on Solid Support Richter, H.; Jung, G. Tetrahedron Lett. 1998, 39, 2729-2730.

4.2.34. Copper-Catalyzed Coupling of Polymer Bound Iodide with Organostannanes Kang, S.-K.; Kim, J.-S.; Yoon, S.-K.; Lim, K.-H.; Yoon, S. S. Tetrahedron Lett. 1998, 39, 3011-3012.

4.2.35. The Solid Phase Synthesis of Complex Propargylamines Using the Combination of Sonogashira and Mannich Reactions Dyatkin, A. B.; Rivero, R. A. Tetrahedron Lett. 1998, 39, 3647-3650.

4.2.36. The Stille Cross Coupling Reactions on Solid Support. Link to Solution Phase Directed ortho Metalation. An Ester Linker Approach to Styryl, Biaryl and Heterobiaryl Carboxylic Acids Chamoin, S.; Houldsworth, S.; Snieckus, V. Tetrahedron Lett. 1998, 39, 4175-4178.

4.2.37. The Suzuki-Miyaura Cross Coupling Reactions on Solid Support. Link to Solution Phase Directed ortho Metalation. The Leznoff Acetal Linker Approach to Biaryl and Heterobiaryl Aldehydes Chamoin, S.; Houldsworth, S.; Kruse, C. G.; Bakker, W. I.; Snieckus, V. Tetrahedron Lett. 1998, 39, 4179-4182.

4.2.38. Diels-Alder Reaction on Solid Supports Using Polymer-Bound Oxazolidinones Winkler, J. D.; McCoull, W. Tetrahedron Lett. 1998, 39, 4935-4936.

4.2.39. Directed ortho-Lithiation on Solid Phase Havez, S.; Begtrup, M.; Vedso, P.; Anderson, K.; Ruhland, T. J. Org. Chem. 1998, 63, 7418-7420.

4.2.40. Solid-Phase Horner-Emmons Synthesis of Olefins Salvino, J. M.;  Kiesow, T. J.; Darnbrough, S.; Labaudiniere, R. J. Combinatorial Chemistry 1999, 1, 2, 134-139.

4.2.41. Intermolecular Conjugate Addition of Alkyl Radicals on Solid Phase Zhu, X.; Ganesan, A. J. Combinatorial Chemistry 1999, 1, 2, 157-162.

4.2.42. New Chemoselective Metalating Agents for Solid-Phase Synthesis Kondo, Y.; Komine, T.; Fujinami, M.; Uchiyama, M.; Sakamoto, T. J. Combinatorial Chemistry 1999, 1, 1, 123-126.

4.2.43. Palladium-Catalyzed Coupling of Functionalized Bromoarenes to a Polystyrene-Bound Aryl Tributylstannane Brody, M. S.; Finn, M. G. Tetrahedron Lett. 1999, 40, 3, 415-418.

4.2.44. Novel Synthesis of alpha-Amino Acid Derivatives through Triethylborane-Induced Solid-Phase Radical Reactions Miyabe, H.; Fujishima, Y.; Naito, T. J. Org. Chem. 1999, 64, 2174-2175.  

4.2.45.  Pd-Mediated C-C and Cs Bond Formation with Olefins and Acetylenes on Solid Support - A Scope and Limitations Study Berteina, S.; Wendeborn, S.; Brill, W. K. D., and Demesmaeker, A. Synlett. 1998;6, 676-678.

4.2.46. Radical and Palladium-Mediated Cyclizations of Ortho-Iodo Benzyl Enamines - Application to Solid-Phase Synthesis Berteina, S.; Wendeborn, S., and Demesmaeker, A. Synlett 1998; 11, 1231-1233.

4.2.47. Synthesis of homoallylic amines via N-acyliminium ion reactions on solid support W. J. N. Meester, F. P. J. T. Rutjes, P. H. H. Hermkens, H. Hiemstra, Tetrahedron Lett. 1999, 40(8), 1601-1604.

4.2.48. Allylindium and allylboronic acid pinacolate: mild reagents for the allylation of resin-bound aldehydes. Application to the solid-phase synthesis of hydroxypropylamines C. L. Cavallaro, T. Herpin, B. F. McGuinness, Y. C. Shimshock, R. E. Dolle, Tetrahedron Lett. 1999, 40(14), 2711-2714.

4.2.49. Preparation of new functionalized hydrocarbon linkers via Suzuki cross coupling reaction C. Vanier, A. Wagner, C. Mioskowski, Tetrahedron Lett. 1999, 40(23), 4335-4338.

4.2.50. Solid-phase synthesis of amino acids by radical addition to a dehydroalanine derivative A.-M. Yim, Y. Vidal, P. Viallefont, J. Martinez, Tetrahedron Lett. 1999, 40(24), 4535-4538.

4.2.51. Stereocontrolled solution and solid phase enolate alkylations and hydroxylations generation of three and four contiguous stereogenic carbon atoms in acyclic systems S. Hanessian, J. Ma, W. Wang, Tetrahedron Lett. 1999, 40(25), 4631-4634.

4.2.52. Solid-Phase Synthesis of -Keto Esters via Sequential Baylis-Hillman and Heck Reactions Kulkarni, B. A., Ganesan, A., J. Comb. Chem.; 1999;1(5); 373-378.

4.2.53. A Novel Chiral Pentamine Ligand for Enantioselective -Alkylation of Acyclic Lithium Amide Enolates. Optimization of Chiral Ligands for Asymmetric Reactions Using Solid-Phase Organic Synthesis Matsuo, J.-i., Odashima, K., Kobayashi, S. Org. Lett. 1999; 1(2); 345-348.

4.2.54. Solid-phase synthesis of unnatural alpha-amino acid derivatives using a resin-bound glycine cation equivalent M. J. O'Donnell, F. Delgado, M. D. Drew, R. S. Pottorf, C. Zhou, W. L. Scott Tetrahedron Lett.1999,40(32), 5831-5836.

4.2.55. Palladium-catalyzed three component coupling on solid support Y. Wang, T.-N. Huang Tetrahedron Lett. 1999, 40(32), 5837-5840.

4.2.56. Two Methods for the Preparation of 2-Cyclohexenones from Resin-Bound 1,3-Cyclohexanedione Fraley, M. E.; Rubino, R. S. Tetrahedron Lett. 1997, 38, 3365-3368.

4.2.57. Solid-Phase Synthesis on Planar Supports Lebl, M.Biopolymers (Peptide Science) 1998, 47, 397-404.

4.2.58. Ring-Closing Metathesis on Solid Support - Elaboration of a Cyclization/Cleavage Strategy

Towards Unsaturated Alpha-Ester-Substituted N-Heterocycles Veerman, J. J. N.; Vanmaarseveen, J. H.; Visser, G. M.; Kruse, C. G.; Schoemaker, H. E.; Hiemstra, H., and Rutjes, F. P. J. T. Eur. J. Org.Chem. 1998; (11) 2583-2589

4.2.59. Resin type can have important effects on solid phase asymmetric reactions alkylation reactions Burgess, K., & Lim, D. J. Chem. Soc. Chem. Commun. 1997, 785-786.

4.2.60. Ruthenium catalyzed cross metathesis binding of functionalized olefins to polystyrene resin via a novel allylsilyl linker suitable for electrophilic cleavage Schuster, M., Lukas, N., & Blechert, S. J. Chem. Soc. Chem. Commun. 1997, 823-824.

4.2.61. Chameleon Catches in Combinatorial Chemistry - Tebbe Olefination of Polymer-Supported Esters and the Synthesis of Amines, Cyclohexanones, Enones, Methyl Ketones and Thiazoles Ball, C. P.; Barrett, A. G. M.; Commercon, A.; Compere, D.; Kuhn, C.; Roberts, R. S.; Smith, M. L., and Venier, O. Chem. Comm. 1998, (18) 2019-2020.

4.2.62. Palladium-catalyzed allylic substitution on solid support Tietze, L.F., Hippe, T., & Steinmetz, A. Chem. Commun. 1998, 793-794.

4.2.63. Development of Chloromethylated SynPhase Crowns and Their Use in Pd(0) Mediated Cross-Coupling Reactions Wendeborn, S., Beaudegnies, R., Ang, K.H., Maeji, N. J. Biotech. Bioeng. (Comb.Chem.) 1998, 61, 89-92.

4.2.64. Synthesis of benzofuran derivatives on solid support via SmI2-mediated radical cyclization Du, X., Armstrong, R. J. Org. Chem. 1997, 62, 5678-5679.

4.2.65. Resin-to-resin acyl- and aminoacyl-transfer reactions using oxime supports Hamuro, Y., Scialdone, M. A., DeGrado, W. F. J. Amer. Chem. Soc. 1999, 121, 1636-1644.

4.2.66. An approach to controlled oligomerization via iterative Diels-Alder cycloadditions on solid supports Winkler, J.D., Kwak, Y.S. J. Org. Chem. 1998, 63, 8634-8635.

4.2.67. Preparation of Highly Functionalized Grignard-Reagents by an Iodine-Magnesium Exchange-Reaction and Its Application in Solid-Phase Synthesis Boymond, L.; Rottlander, M.; Cahiez, G.; Knochel, P. Angew. Chem. Int. Ed. 1998; 37(12) 1701-1703.

4.2.68. Palladium-catalyzed carbon-carbon bond formation on a solid phase utilizing hypervalent iodonium salts Kang, S.K.; Yoon, S.K.; Lim, K.H.; Son, H.J.; Baik, T.G. Syn. Commun. 1998, 28, 3645-3655.

4.2.69. Polymer-supported acetylide addition to hexa-2,4-dienal Blaskovich, M.A.; Kahn, M. Synthesis-Stuttgart 1998, 965-966.

4.2.70. Mild N-Dealkylation of Tertiary, Benzylic Amines with Acid Chlorides: Applications to Solid Phase Chemistry Miller, M. W.; Vice, S. F.; McCombie, S. W. Tetrahedron Lett. 1998, 39, 3429-3432.

4.2.71. Solid phase synthesis of cyclopropenes Cano, M.; Camps, F.; Joglar, J. Tetrahedron Lett. 1998, 39, 9819-9822.

4.2.72. Ring closing metathesis in organic synthesis: Evolution of a high speed, solid phase method for the preparation of -turn mimetics Piscopio, A. D.; Miller, J. F.; Koch, K. Tetrahedron 1999, 55(27), 8189-8198.

4.2.73. Solution-phase ring opening cross-metathesis of bicyclic alkenes with styrene derivatives and its application to "resin capture" solid-phase synthesis Cuny, G. D.; Cao, J.; Sidhu, A.; Hauske, J. R. Tetrahedron 1999, 55(27), 8169 -8178.

4.2.74. Chiral lithium amides on solid support: synthesis and applications in enantioselective deprotonation of cyclic ketones Majewski, M.; Ulaczyk, A.; Wang, F. Tetrahedron Lett. 1999, 40(50), 8755.

4.2.75. Enantioselective solid-phase synthesis of a-amino acid derivatives O'Donnell, M. J.; Delgado, F.; Pottorf, R. S. Tetrahedron, 1999, 55(20), 6347-6362.

4.2.76. Solid phase approach to muscone synthesis: Rh(I)-catalyzed hydroformylation of a 1,1-disubstituted alkene on the multipinTM system Takahashi, T.; Ebata, S.; Doi, T. Tetrahedron Lett. 1998, 39, 1369-1372.

4.2.77. Soluble polymer-supported synthesis of arylpiperazines Pan, P.-C.; Sun, C.-M. Tetrahedron Lett. 1998, 39, 9505-9508.

4.2.78. Highly stereoselective preparation of 3,3-disubstituted acrylates on polyethylene glycol Blettner, C.G.; Konig, W.A.; Stenzel, W.; Schotten, T. Tetrahedron Lett. 1999, 40, 2101-2102.

4.2.79. An easily prepared, air and moisture stable, resin-bound palladium catalyst for Suzuki cross-coupling reactions Zhang, T. Y.; Allen, M. J. Tetrahedron Lett. 1999, 40(32), 5813-5816.

4.2.80. Palladium-catalyzed three component coupling on solid support Wang, Y.; Huang, T.-N. Tetrahedron Lett. 1999, 40(32), 5837-5840.

4.2.81. Solid-Phase Intermolecular Radical Reactions 1. Sulfonyl Radical Addition to Isolated Alkens and Alkynes Caddick, S.; Hamza, D.; Wadman, S. N. Tetrahedron Lett. 1999, 40, 7285-7288.

4.2.82. Exploring the Scope of Poly(ethylene glycol) (PEG) as a Soluble Polymer Matrix for the Stille Cross-Coupling Reaction Sieber, F.; Wentworth, P. Jr.; Janda, K. D. Journal of Combinatorial Chemistry 1999, 1(6), 540-546.

4.2.83. Parallel Synthesis of Prostaglandin E1 Analogues Dragoli, D. R; Thompson, L. A. O'Brien, J.; Ellman, J. A. Journal of Combinatorial Chemistry; 1999, 1(6), 534-539.
 
 

4.3. Mitsunobu Reactions on Solid Support

4.3.1. Solid-Phase Synthesis of Smale Molecule Libraries using Double Combinatorial Chemistry Nielsen, J.; Jensen, F. R. Tetrahedron Lett. 1997, 38, 2011-2014.

4.3.2. Solid Phase Synthesis of Fmoc N-Methyl Amino Acids: Application of the Fukuyama Amine Synthesis Yang, L.; Chiu, K. Tetrahedron Lett. 1997, 38, 7307-7310.

4.3.3. Amino Acid Side Chain Attachment Approach and Its Application to the Synthesis of Tyrosine-Containing Cyclic Peptides Cabrele, C.; Langer, M.; Beck-Sickinger, A. G. J. Org. Chem. 1999, 64, 12, 4353-4361.

4.3.4. A novel solid support for derivatization and subsequent N-alkylation of secondary amines: Preparation of N-alkylated 5- and 6-alkoxy-1,2,3,4-tetrahydroisoquinolines via Mitsunobu reaction Heinonen, P., Lonnberg, H. Tetrahedron Lett. 1997, 38, 8569-8572.
 
 

4.4. Substitution and Addition Reactions on Solid Support

4.4.1. Site-Selective N-Methylation of Peptides on Solid Support Miller, S. C.; Scanlan, T. S. J. Am. Chem. Soc. 1997, 119, 2301-2302.

4.4.2. Rapid and Efficient Solid Phase Synthesis of Cyclic Peptides with Endocyclic Biaryl Ether Bonds Burgess, K.; Lim, D.; Bois-Choussy, M.; Zhu, J. Tetrahedron Lett. 1997, 38, 3345-3348.

4.4.3. Mannich Reactions of a Resin-Bound Terminal Alkyne Youngman, M. A.; Dax, S. L. Tetrahedron Lett. 1997, 38, 6347-6350.

4.4.4. The Solid-Phase Combinatorial Synthesis of beta-Thioketones Chen, C.; Randall, L. A. A.; Miller, R. B.; Jones, A. D.; Kurth, M. J. Tetrahedron 1997, 53, 6595-6609.

4.4.5. Solid Phase Synthesis of beta-Peptoids: N-Substituted beta-Aminopropionic Acid Oligomers Hamper, B. C.; Kolodziej, S. A.; Scates, A. M.; Smith, R. G.; Cortez, E. J. Org. Chem. 1998, 63, 708-718.

4.4.6. Solid Phase Synthesis of Unsymmetrical Secondary Amines-Application to the Synthesis of Arylethanolamines and Arylpropanolamines Purandare, A. V.; Poss, M. A. Tetrahedron Lett. 1998, 39, 935-938.

4.4.7. oNBS-SPPS: A New Method for Solid-Phase Peptide Synthesis Miller, S. C.; Scanlan, T. S. J. Am. Chem. Soc. 1997, 120, 2690-2691.

4.4.8. Site-Specific N-Alkylation of Peptides on Solid Phase Reichwein, J. F.; Liskamp, R. M. J. Tetrahedron Lett. 1998, 39, 1243-1246.

4.4.9. Solid Phase Synthesis of Functional Biaryl Ethers: Versatile Scaffolds for Combinatorial Chemistry Wijkmans, J. C. H. M.; Culshaw, A. J.; Baxter, A. D. Molecular Diversity 1998, 3, 117-120.

4.4.10. Composition and Purity of Combinatorial Aryl Ether Collection Analyzed by Electrospray Mass Spectrometry Haap, W. J.; Metzger, J. W.; Kempter, C.; Jung, G. Molecular Diversity 1998, 3, 29-41.

4.4.11. Rapid Solid Phase Synthesis of alpha-Amino Acids Barbaste, M.; Rolland-Fulcrand, V.; Roumestant, M.-L.; Viallefont, P.; Martinez, J. Tetrahedron Lett. 1998, 39, 6287-6290.

4.4.12. A Simple and Efficient Method for the Syntheses of Thioether Cyclic Peptides Yu, L.; Lai, Y.; Wade, J. V.; Coutts, S. M. Tetrahedron Lett. 1998, 39, 6633-6636.

4.4.13. First Aromatic Electrophilic Iodination Reaction on the Solid-Phase: Iodination of Bioactive Peptides Arsequell, G.; Espuna, G.; Valencia, G.; Barluenga, J.; Carlon, R. P.; Gonzalez, J. M. Tetrahedron Lett. 1998, 39, 7393-7396.

4.4.14. Composition and Purity of Combinatorial Aryl Ether Collections Analyzed by Electrospray Mass Spectrometry (Williamson etherification) Haap, W. J.; Metzger, J. W.; Kempter, C.; Jung, G. Molecular Diversity 1997, 3, 29-41.

4.4.15. Toxicity and osmoprotective activities of analogues of glycine betaine obtained by solid phase organic synthesis towards Sinorhizobium meliloti Cosquer, A.; Pichereau, V.; Le Mee, D.; Le Roch, M.; Renault, J.; Carboni, B.; Uriac, P.; Bernard, T. Bioorganic & Medicinal Chemistry Letters, 1999 9, 1, 49-54.

4.4.16. Solution and Solid-Phase p-Alkoxybenzylation of Alcohols Under Neutral Conditions Hanessian, S.; Huynh, H. K. Tetrahedron Letters, 1999, 40, 4, 671-674.

4.4.17. Solid supported aryl/heteroaryl C-N cross-coupling reactions A. P. Combs, S. Saubern, M. Rafalski, P. Y. S. Lam Hiemstra, Tetrahedron Lett. 1999, 40, 9, 1623-1626.

4.4.18. Model Study for Preparation of Asymmetric N,N'-Disubstituted Piperazine Library - Efficient Synthesis of Aryl Piperazine and Benzyl Piperazine Derivatives on the Solid Support Yamamoto, Y.; Ajito, K., and Ohtsuka, Y. Chem. Lett. 1998; (5):379-380.

4.4.19. Efficient Solid-Phase Synthesis of Beta-Aminosubstituted Piperidinols Rosse, G.; Ouertani, F.; Schroder, H. J. Combinatorial Chemistry 1999, 1, 5, 397-401.

4.4.20. One Pot Synthesis of Unsymmetrically Functionalized Polyamines by a Solid Phase Strategy Starting from their Symmetrical Polyamine-Counterparts Byk G.; Frederic, M.; Scherman, D Tetrahedron Lett. 1997, (38), 3219-3222.

4.4.21. A Visual Tagging Process for Mix and Sort Combinatorial Chemistry Guiles, J. W.; Lanter, C. L.; Rivero, R. A. Angew. Chem. Int. Ed. 1998; 37(7) 926-928.

4.4.22. Application of polymer-supported electrophilic reagents for the 1,2-functionalization of glycals Kirschning, A.; Jesberger, M.; Monenschein, H. Tetrahedron Lett. 1999, 40(51), 8999-9002.

4.4.23. Evaluation of Gaseous Hydrogen Fluoride as a Convenient Reagent for Parallel Cleavage from the Solid Support Lebl, M.; Pires, J.; Poncar, P.; Pokorny, V Journal of Combinatorial Chemistry; 1999, 1(6), 474-479.

4.4.24. Synthesis and Use of a 2-(Trimethylsilyl)ethoxymethyl-Based Linker in Solid-Phase Organic Chemistry Koot, W.-J.Journal of Combinatorial Chemistry 1999, 1(6), 467-473.
 
 

4.5. Oxidations on Solid Support

4.5.1. Ozone: a Versatile Reagent for Solid Phase Synthesis Sylvain, C. Wagner, A.; Mioskowski, C. Tetrahedron Lett. 1997, 38, 1043-1044.

4.5.2. Synthesis of Functionalized gamma- and delta-Lactones via Polymer-Bound Epoxides Hetet, C. L.; David, M.; Carreaux, F.; Carboni, B.; Sauleau, A. Tetrahedron Lett. 1997, 38, 5153-5156.

4.5.3. Solid-Phase Synthesis of Tyrosine Peptide Aldehdyes.  Analogues of (S)-MAPI Page, P.; Bradley, M.; Walters, I.; Teague, S. J. Org. Chem. 1999, 64, 794-799.

4.5.4. Solid phase synthesis of aryl and aryl amines using the Curtius rearrangement S. Sunami, T. Sagara, M. Ohkubo, H. Morishima Hiemstra, Tetrahedron Lett. 1999, 40, 9, 1721-1724.

4.5.5. Selective solid-phase iodination of phenolic groups with bis(pyridine)iodonium (I) tetrafluoroborate G. Arsequell, G. Espuña, G. Valencia, J. Barluenga, R. Pérez Carlón, J. M. González Tetrahedron Lett., 1999, 40, 7279-7282.

4.5.6. Polyaniline Supported Cobalt(II) Catalyst: Oxidation of Alkenes with Molecular Oxygen Das, B. C.; Iqbal, J. Tetrahedron Lett., 1997, 38, 1235-1238.

4.5.7. High-throughput purification of solution-phase periodinane mediated oxidation reactions utilizing a novel thiosulfate resin Parlow, J. J.;. Case, B. L.; South, M. S. Tetrahedron, 1999, 55(22), 6785-6796.
 
 

4.6. Reductions on Solid Support

4.6.1. Alkylation of Rink's Amide Linker on Polystyrene Resin: A Reductive Amination Approach to Modified Amine-Linkers for the Solid Phase Synthesis of N-Substituted Amide Derivatives Brown, E. G.; Nuss, J. M. Tetrahedron Lett. 1997, 38, 8457-8460.

4.6.2. Potassium Borohydride Reductions of Immobilised Ketosteroids Briggs, J. C.; Hodge, P.; Zhengpu, Z. Tetrahedron 1997, 53, 3943-3956.

4.6.3. Solid Phase Synthesis of N-Carboxy Alkyl-Containing Peptides Derived from Enantiopure Alpha-Keto-Beta-Amino Acids Fernandez-Garcia, C.; Prager, K.; McKervey, M. A.; Walker, B.; Williams, C. H. Bioorg. Med. Chem. Lett. 1998, 8, 433-436.

4.6.4. Reductions of Olefins on Solid Support Using Diimide Lacombe, P.; Castagner, B.; Gareau, Y.; Ruel, R. Tetrahedron Lett. 1998, 39, 6785-6786.

4.6.5. Titanium Mediated Reductive Amination on Solid Support:  Extending the Utility of the 4-Hydroxy-Thiophenol Linker Breitenbucher, J. G.; Hui, H. C. Tetrahedron Lett. 1998, 39, 8207-8210.

4.6.6. Efficiencies of Reductive Amination Reactions on Different Solid Supports Bui, C. T.; Rasoul, F. A.; Ercole, F.; Pham, Y.; Maeji, N. J. Tetrahedron Lett. 1998, 39, 9279-9282.

4.6.7. A New Method for the Mild and Selective Reduction of Aryl Nitro Groups on Solid Support Hari, A.; Miller, B. L. Tetrahedron Lett. 1998, 40, 245-248.

4.6.8. Parallel Solid Phase Synthesis of Tetrasubstituted Diethylenetriamines via Selective Amide Alkylation and Exhaustive Reduction of N-acylated Dipeptides Nefzi, A.; Ostresh, J. M.; Houghten, R. A. Tetrahedron, 1999, 55, 2, 335-344.

4.6.9. Development of a Reductive Alkylation Method Using p-Benzyloxybenzylamine (BOBA) Resin for the Synthesis of N-Alkylated Amides Aoki, Y.; Kobayashi, S. J. Combinatorial Chemistry 1999, 1, 5, 371-372.

4.6.10. Generation of secondary alkyl amines on solid support by borane reduction: Application to the parallel synthesis of PPAR ligands Brown, P.J.; Hurley, K.P.; Stuart, L.W.; Willson, T.M. Synthesis-Stuttgart 1997, 778-782.
 
 

4.7. Preparation of Heterocyclic Compounds

4.7.1. A Solid-Phase Combinatorial Method for the Synthesis of Novel 5- and 6-Membered Ring Lactams Short, K. M.; Mjalli, A. M. M. Tetrahedron Lett. 1997, 38, 359-362.

4.7.2. Combinatorial Synthesis of 2,9-Substituted Purines Gray, N. S.; Kwon, S.; Schultz, P. G. Tetrahedron Lett. 1997, 38, 1161-1164.

4.7.3. Construction of Indole and Benzofuran Systems on Solid-Phase via Palladium Mediated Cyclizations Zhang, H-C.; Maryanoff, B. E. J. Org. Chem. 1997, 62, 1804-1809.

4.7.4. Synthesis of Trisubstituted Indoles on the Solid Phase via Palladium-Mediated Heteroannulation of Internal Alkynes Zhang, H-C.; Brumfield, K. K.; Maryanoff, B. E. Tetrahedron Lett. 1997, 38, 2439-2442.

4.7.5. Solid Phase Synthesis of 2-Substituted Benzofurans via the Palladium-Catalysed Heteroannulation of Acetylenes Fagnola, M. C.; Candiani, I.; Visentin, G.; Cabri, W.; Zarini, F.; Mongelli, N.; Bedeschi, A. Tetrahedron Lett. 1997, 38, 2311-2314.

4.7.6. Solid-Phase Synthesis of Indoles Using the Palladium-Catalysed Coupling of Alkynes with Iodoaniline Derivatives Fancelli, D.; Fagnola, M. C.; Severino, D.; Bedeschi, A. Tetrahedron Lett. 1997, 38,2307-2310.

4.7.7. A General and Efficient Solid Phase Synthesis of Quinazoline-2,4-diones Gordeev, M. F.; Hui, H. C.; Gordon, E. M.; Patel, D. V. Tetrahedron Lett. 1997, 38, 1729-1732.

4.7.8. Combinatorial Synthesis and Biological Evaluation of Library of Small-Molecule Ser/Thr-Protein Phosphatase Inhibitors Wipf, P.; Cunningham, A.; Rice, R. L.; Lazo, J. S. Bioorg. Med. Chem. 1997, 5, 165-177.

4.7.10. Combinatorial Synthesis of Heterocycles: Solid Phase Synthesis of 2-Arylquinoline-4-carboxylic Acid Derivatives Gopalsamy, A.; Pallai, P. V. Tetrahedron Lett. 1997, 38, 907-910.

4.7.11. Solid Phase Synthesis of Heterocyclic Compounds from Linear Peptides: Cyclic Ureas and Thioureas Nefzi, A.; Ostresh, J. M.; Meyer, J-P.; Houghten, R. A. Tetrahedron Lett. 1997, 38, 931-934.

4.7.12. Solid Phase Synthesis of Biphenyltetrazole Derivatives Yoo, S.; Seo, J.; Yi, K.; Gong, Y. Tetrahedron Lett., 1997, 38, 1227-1230.

4.7.13. An Investigation into Solid-Phase Radical Chemistry-Synthesis of Furan Rings Routledge, A.; Abell, C.; Balasubramanian, S. Synlett 1997, 1, 61-62.

4.7.14. Solid Phase Synthesis of Heterocyclic Compounds from Linear Peptides: Cyclic Ureas and Thioureas Nefzi, A.; Ostresh, J. M.; Meyer, J-P.; Houghten, R. A. Tetrahedron Lett. 1997, 38, 931-934.

4.7.15. Solid Phase Synthesis of Hydantoin Library Using a Novel Cyclization and Traceless Cleavage Step Kim, S. W.; Ahn, S. Y.; Koh, J. S.; Lee, J. H.; Ro, S.; Cho, H. Y. Tetrahedron Lett. 1997, 38, 4603-4606.

4.7.16. Solid Phase Synthesis of 3,4-Disubstituted-7-carbamoyl-1,2,3,4-tetrahydroquinoxalin-2-ones Lee, J.; Murray, W. V.; Rivero, R. A. J. Org. Chem. 1997, 62, 3874-3879.

4.7.17. Two Methods for the Preparation of 2-Cyclohexenones from Resin-Bound 1,3-Cyclohexanedione Fraley, M. E.; Rubino, R. S. Tetrahedron Lett. 1997, 38, 3365-3368.

4.7.18. Synthesis of 4-Amino-3,4-dihydro-2(1H)-Quinolinones via beta-Lactam Intermediates on The Solid Phase Pei, Y.; Houghten, R. A.; Kiely, J. S. Tetrahedron Lett. 1997, 38, 3349-3352.

4.7.19. Rapid and Efficient Solid Phase Syntheses of Cyclic Peptides with Endocyclic Biaryl Ether Bonds Burgess, K.; Lim, D.; Bois-Choussy, M.; Zhu, J. Tetrahedron Lett. 1997, 38, 3345-3348.

4.7.20. Solid Phase Synthesis of 2,3-Dihydro-4-pyridones: Reaction of Danishefsky's Diene with Polymer-Bound Imines Wang, Y.; Wilson, S. R. Tetrahedron Lett. 1997, 38, 4021-4024.

4.7.21. Solid Phase Synthesis of 1,2,4,7-Tetrasubstituted Perhydro-1,4-diazepine-2,5-diones Nefzi, A.; Ostresh, J. M.; Houghten, R. A. Tetrahedron Lett. 1997, 38, 4943-4946.

4.7.22. Resin-Bound Isothiocyanates and Their Synthetic Equivalents as Intermediates for the Solid-Phase Synthesis of Substituted Thiophenes Stephensen, H.; Zaragoza, F. J. Org. Chem. 1997, 62, 6096-6097.

4.7.23. Cyclobutenedione Derivatives on Solid Support: Toward Multiple Core Structure Libraries Tempest, P. A.; Armstrong, R. W. J. Am. Chem. Soc. 1997, 119, 7607-7608.

4.7.24. Solid-Phase Synthesis of 1,4-Benzodiazepine-2,5-diones. Library Preparation and Demonstration of Synthesis Generality Boojamra, C. G.; Burow, K. M.; Thompson, L. A.; Ellman, J. A. J. Org. Chem. 1997, 62, 1240-1256.

4.7.25. The Synthesis of a 1680 Member 1,4-Benzodiazepine Library Bunin, B. A.; Plunkett, M. J.; Ellman, J. A.; Bray, A. M. New J. Chem. 1997, 21, 125-130.

4.7.26. Solid Phase Synthesis of Benzimidazoles Phillips, G. B.; Wei, G. P. Tetrahedron Lett. 1997, 37, 4887-4890.

4.7.27. Solid-Phase Synthesis of Benzoxazoles via Mitsunobu Reaction Wang, F.; Hauske, J. R. Tetrahedron Lett. 1997, 38, 6529-6532.

4.7.28. Solid-Phase Synthesis of Pyrrolidines via 2-Azaallyl Anion Cycloadditions with Alkenes Pearson, W. H.; Clark, R. B. Tetrahedron Lett. 1997, 38, 7669-7672.

4.7.29. Synthesis of Epothilones A and B in Solid and Solution Phase Nicolaou, K. C.; Winssinger, N.; Pastor, J.; Ninkovic, S.; Sarabia, F.; He, Y.; Vourloumis, D.; Yang, Z.; Li, T.; Giannakakou, P.; Hamel, E. Nature, 1997, 387, 268-272.

4.7.30. Encoded Combinatorial Chemistry: Synthesis and Screening of a Library of Highly Functionalized Pyrrolidines Maclean, D.; Schuller, J. R.; Murphy, M. M.; Ni, Z.-J.; Gordon, E. M.; Gallop, M. A. Proc. Natl. Acad. Sci. USA 1997, 94, 2805-2810.

4.7.31. Beta-Lactams on Solid Support: Mild and Efficient Removal of Penicillin Derivatives from Merrifield Resin using Aluminum Chloride Mata, E. G. Tetrahedron Lett. 1997, 38, 6335-6338.

4.7.32. Synthesis of 2-Oxindole Derivatives via the Intramolecular Heck Reaction on Solid Support Arumugam, V.; Routledge, A.; Abell, C.; Balasubramanian, S. Tetrahedron Lett. 1997, 38, 6473-6476.

4.7.33. The Solid Phase Synthesis of Tri-Substituted Indoles Ellingboe, J. W.; Collini, M. D. Tetrahedron Lett. 1997, 38, 7963-7966.

4.7.34. Solid Support Synthesis of Tetrahydroquinolines via the Grieco Three Component Condensation Kiselyov, A. S.; Armstrong, R. W. Tetrahedron Lett. 1997, 38, 6163-6166.

4.7.35. Solid Phase Synthesis of Quinazolinones Mayer, J. P.; Lewis, G. S.; Curtis, M. J.; Zhang, J. Tetrahedron Lett. 1997, 38, 8445-8448.

4.7.36. Synthetic Design for Combinatorial Chemistry. Solution and Polymer-Supported Synthesis of Polycyclic Lactams by Intramolecular Cyclization of Azomethine Ylides Marx, M. A.; Grillot, A.-L.; Louer, C. T.; Beaver, K. A.; Bartlett, P. A. J. Am. Chem. Soc. 1997, 119, 6153-6167.

4.7.37. Solid-Phase Synthesis of Diverse Tetrahydro-1,4-Benzodiazepine-2-ones Bhalay, G.; Blaney, P.; Palmer, V. H.; Baxter, A. D. Tetrahedron Lett. 1997, 38, 8375-8378.

4.7.38. A Chemoselective Rhodium(II) Mediated Solid Phase 1,3-Dipolar Cycloaddition and its Application to a Thermally Self-Cleaving Furan Scaffold Whitehouse, D. L.; Nelson, K. H.; Savinov, S. N.; Austin, D. J. Tetrahedron Lett. 1997, 38, 7139-7142.

4.7.39. "Traceless" Solid-Phase Synthesis of Furans via 1,3-Dipolar Cycloaddition Reactions of Isomuchnones Gowravaram, M. R.; Gallop, M. A. Tetrahedron Lett. 1997, 38, 6973-6976.

4.7.40. Solid Phase Synthesis of Fused Bicyclic Amino Acid Derivatives via Intramolecular Pauson-Khand Cyclization: Versatile Scaffolds for Combinatorial Chemistry Bolton, G. L.; Hodges, J. C.; Rubin, J. R. Tetrahedron 1997, 53,6611-6634.

4.7.41. Polymer-Supported Synthesis as a Tool for Improving Chemoselectivity: Pauson-Khand Reaction Spitzer, J. L.; Kurth, M. J.; Schore, N. E.; Najdi, S. D. Tetrahedron 1997, 53, 6791-6808.

4.7.42. Exploitation of the Ugi 4CC Reaction: Preparation of Small Molecule Combinatorial Libraries via Solid Phase Short, K. M.; Ching, B. W.; Mjalli, A. M. M. Tetrahedron 1997, 53, 6653-6679.

4.7.43. Solid-Phase Synthesis of beta-Sultams Gordeev, M. F.; Gordon, E. M.; Patel, D. V. J. Org. Chem. 1997, 62, 8177-8181.

4.7.44. Solid-Phase Synthesis of 2-Aminothiazoles Kearney, P. C.; Fernandez, M.; Flygare, J. A. J. Org. Chem. 1997, 62, 196-200.

4.7.45. Synthesis of Dihydropyridone Scaffolds on solid Support: Resin Activation/Capture Approach/REACAP Technology Chen, C.; McDonald, I. A.; Munoz, B. Tetrahedron Lett. 1998, 38, 217-220.

4.7.46. A Novel and Efficient Approach for the Combinatorial Synthesis of Structurally Diverse Pyrimidines on Solid Support Obrecht, D.; Abrecht, C.; Grieder, A.; Villalgordo, J. M. Helv. Chem. Acta. 1997, 80, 65-72.

4.7.47. Solid-Phase Synthesis of 3,4-Dihydroquinazoline Wang, F.; Hauske, J. R. Tetrahedron Lett. 1997, 38, 8651-8654.

4.7.48. Solid Phase Synthesis of 5-Aminopyrazoles and Derivatives Watson, S. P.; Wilson, R. D.; Judd, D. B.; Richards, S. A. Tetrahedron Lett. 1997, 38, 9065-9068.

4.7.49. Xanthines as a Scaffold for Molecular Diversity Heizmann, G.; Eberle, A. N. Molec. Div. 1996, 2, 171-174.

4.7.50. Solid-Phase Synthesis of Polymer-Bound beta-Ketoesters and Their Application in the Synthesis of Structurally Diverse Pyrazolones Tietze, L. F.; Steinmetz, A.; Balkenhohl, F. Bioorg. Med. Chem. Lett. 1997, 7, 1303-1306.

4.7.51. The Solid Phase Synthesis of Trisubstituted 1,4-Diazabicyclo[4.3.0]nonan-2-one Scaffolds: On Bead Monitoring of Heterocycle Forming Reactions Using N-15 NMR Swayze, E. E. Tetrahedron Lett. 1997, 38, 8643-8646.

4.7.52. Key Intermediates in Combinatorial Chemistry: Access to Various Heterocycles from alpha,beta-Unsaturated Ketones on the Solid Phase Marzinzik, A. L.; Felder, E. R. J. Org. Chem. 1998, 63, 723-727.

4.7.53. Solid-Phase Synthesis of Isoxazolines Cheng, J. F.; Mjalli, A. M. M. Tetrahedron Lett. 1998, 39, 939-942.

4.7.54. Solid Phase Synthesis of Tropane Derivatives Jonsson, D.; Molin, H.; Unden, A. Tetrahedron Lett. 1998, 39, 1059-1062.

4.7.55. A Peptoid Based Synthesis of Di- and Tri-Substituted 2-Oxopiperazines on Solid Support Goff, D. A. Tetrahedron Lett. 1998, 39, 1473-1476.

4.7.56. The Synthesis of 2-Imidazolidones on Solid Support by Tandem Aminoacylation/Michael Addition Goff, D. A. Tetrahedron Lett. 1998, 39, 1477-1480.

4.7.57. Generation of a Piperazine-2-carboxamide Library: A Practical Application of the Phenol-Sulfide React and Release Linker Breitenbucher, J. G.; Johnson, C. R.; Haight, M.; Phelan, J. C. Tetrahedron Lett. 1998, 39, 1295-1298.

4.7.58. Synthesis of Diverse Tetrahydro-beta-Carboline-3-Carboxamides and -2,3-Bis-lactams On a Versatile 4-Hydroxythiophenol-Linked Solid Support Fantauzzi, P. P.; Yager, K. M. Tetrahedron Lett. 1998, 39, 1291-1294.

4.7.59. Solid-Phase Synthesis of Diverse E- and F-Series Prostaglandins Thompson, L. A.; Moore, F. L.; Moon, Y-C.; Ellman, J. A. J. Org. Chem. 1998, 63, 2066-2067.

4.7.60. Solid-Supported Synthesis of Imidazoles: A Strategy for Direct Resin-Attachment to the Imidazole Core Bilodeau, M. T.; Cunningham, A. M. J. Org. Chem. 1998, 63, 2800-2801

4.7.61. Carbohydrate-Based Small-Molecule Scaffolds for the Construction of Universal Pharmacophore Mapping Libraries Sofia, M. J.; Hunter, R.; Chan, T. Y.; Vaughan, A.; Dulina, R.; Wang, H.; Gange, D. J. Org. Chem. 1998, 63, 2802-2803.

4.7.62. Solid-Phase Synthesis: Intramolecular Azomethine Ylide Cycladdition (-Proline) and Carbanilide Cyclization (-Hydantoin) Reactions Gong, Y.-D.; Najdi, S.; Olmstead, M. M.; Kurth, M. J. J. Org. Chem. 1998, 63, 3081-3086.

4.7.63. Solid-Phase Synthesis of Heterocycles Containing an 1-Acyl-3-oxopiperazine Skeleton Vojkovsky, T.; Weichsel, A.; Patek, M. J. Org. Chem. 1998, 63, 3162-3163.

4.7.64. Single Bead IR Monitoring of a Novel Benzimidazole Synthesis Sun, Q.; Yan, B. Bioorg. Med. Chem. Lett. 1998, 8, 361-364.

4.7.65. Facile Substitution of Resin-Bound Indoles via the Mannich Reaction Zhang, H. C.; Brumfield, K. K.; Jaroskova, L.; Maryanoff, B. E. Tetrahedron Lett. 1998, 39, 4449-4452.

4.7.66. Solid-Phase Synthesis of Tetramic Acids Kulkarni, B. A.; Ganesan, A. Tetrahedron Lett. 1998, 39, 4369-4372.

4.7.67. One Pot Solid Phase Synthesis of Isoxazolines Shankar, B. B.; Yang, D. Y.; Girton, S.; Ganguly, A. K. Tetrahedron Lett. 1998, 39, 2447-2448.

4.7.68. Solid-Phase Synthesis of Diketopiperazines, Useful Scaffolds for Combinatorial Chemistry Fresno, M. D.; Alsina, J.; Royo, M.; Barany, G.; Albericio, F. Tetrahedron Lett. 1998, 39, 2639-2642.

4.7.69. Oligosaccharide Synthesis on Controlled-Pore Glass as Solid Phase Material Heckel, A.; Mross, E.; Jung, K. H.; Rademann, J.; Schmidt, R. R. Synlett 1998, 171-173.

4.7.70. A Second Generation Solid Phase Approach to Freidinger Lactams: Application of Fukuyama's Amine Synthesis and Cyclative Release via Ring Closing Metathesis Piscopio, A. D.; Miller, J. F.; Koch, K. Tetrahedron Lett. 1998, 39, 2667-2670.

4.7.71. Cyclic Oligocarbamates Warrass, R.; Wiesmuller, K.-H.; Jung, G. Tetrahedron Lett. 1998, 39, 2715-2716.

4.7.72. Solid Phase Synthesis of 5-Aminopyrazoles and Derivatives Part II Wilson, R. D.; Watson, S. P.; Richards, S. A. Tetrahedron Lett. 1998, 39, 2827-2830.

4.7.73. Solid Phase Synthesis of 2,4-Disubstituted Pyridine and Tetrahydropyridine Derivatives: Resin Activation/Capture Approach/REACAP Technology Chen, C.; Munoz, B. Tetrahedron Lett. 1998, 39, 3401-3404.

4.7.74. High Pressure Promoted Tandem [4+2]/[3+2] Cycloadditions On The Solid Phase Kuster, G. J.; Scheeren, H. W. Tetrahedron Lett. 1998, 39,3613-3616.

4.7.75. Parallel Synthesis of 3-Aminoimidazo[1,2-a]pyridines and pyrazines by a New Three-Component Condensation Blackburn, C.; Guan, B.; Fleming, P.; Shiosaki, K.; Tsai, S. Tetrahedron Lett. 1998, 39, 3635-3638.

4.7.76. Solid Phase Synthesis of 2,4,5-Trisubstituted Thiomorpholin-3-ones Nefzi, A.; Giulianotti, M.; Houghten, R. A. Tetrahedron Lett. 1998, 39, 3635-3638.

4.7.77. Solid Phase Synthesis of a 1,3,5-Trisubstituted Pyridinium Salt Library Lago, M. A.; Nguyen, T. T.; Bhatnagar, P. Tetrahedron Lett. 1998, 39, 3885-3888.

4.7.78. Total Synthesis of a Naturally Occurring Prostaglandin F-2alpha on a Non-Cross-Linked Polystyrene Support Chen, S.; Janda, K. D. Tetrahedron Lett. 1998, 39, 3943-3946.

4.7.79. Solid-Supported Syntheses of 3-Thio-1,2,4-Triazoles Wilson, M. W.; Hernandez, A. S.; Calvet, A. P.; Hodges, J. C. Molecular Diversity1998, 3, 95-112.

4.7.80. Solid Phase Synthesis of Benzamidine and Butylamine-Derived Hydantoin Libraries Kim, S. W.; Koh, J. S.; Lee, E. J.; Ro, S. Molecular Diversity 1998, 3, 129-132.

4.7.81. Combinatorial Approaches to Pharmacophoric Heterocycles: A Solid-Phase Synthesis of 3,1-Benzoxazine-4-Ones Gordeev, M. F. Biotechnology and Bioengineering (Combinatorial Chemistry) 1998, 61, 1, 13-16.

4.7.82. Solid-Phase Synthesis of Substituted Tetramic Acids Matthews, J.; Rivero, R. A. J. Org. Chem. 1998, 63, 4808-4810.

4.7.83.  Solid Phase Synthesis of Fumitremorgin, Verruculogen and Tryprostatin Analogs based on a Cyclization/Cleavage Strategy Loevezijn, A. van; Maarseveen, J. H. van; Stegman, K.; Visser, G. M.; Koomen, G.-J. Tetrahedron Lett. 1998, 39, 4737-4740.

4.7.84. Solid-Phase Synthesis of Substituted Quinoline and Isoquinoline Derivatives Using Heterocyclic N-oxide Chemistry Hoemann, M. Z.; Melikian-Badalian, A.; Kumaravel, G.; Hauske, J. R. Tetrahedron Lett. 1998, 39, 4749-4752.

4.7.85. Solid Phase Synthesis of 1-Aminohydantoin Libraries Wilson, L. J.; Li, M.; Portlock, D. E. Tetrahedron Lett. 1998, 39, 5135-5138.

4.7.86. A Three-Component Solid-Phase Synthesis of 3-Aminoimidazo[1,2-a]azines Blackburn, C. Tetrahedron Lett. 1998, 39, 5469-5472.

4.7.87. Efficient Robotic Synthesis. Multi-component Preparation of a Tricyclic Template by Solid Phase Tsunge Reaction Bicknell, A. J.; Hird, N. W.; Readshaw, S. A. Tetrahedron Lett. 1998, 39, 5869-5872.

4.7.88. Solid-Phase Synthesis of 3-Amino-2-pyrazolines Lyngso, L. O.; Nielsen, J. Tetrahedron Lett. 1998, 39, 5845-5848.

4.7.89. Application of Radical Chemistry to Solid Support Synthesis Berteina, S.; Mesmaeker, A. D. Tetrahedron Lett. 1998, 39, 5759-5762.

4.7.90. Solid-Phase Combinatorial Synthesis of 4-hydroxyquinolin-2(1H)-ones Sim, M. M.; Lee, C. L.; Ganesan, A. Tetrahedron Lett. 1998, 39, 6399-6402.

4.7.91. Solid-Phase Synthesis of Benzimidazoles Mayer, J. P.; Lewis, G. S.; McGee, C.; Bankaitis-Davis, D. Tetrahedron Lett. 1998, 39, 6655-6658.

4.7.92. Combinatorial Chemistry. Use of an Intramolecular Ruthenium Catalyzed Olefin/Alkyne Metathesis Reaction in Tandem With a Diels-Alder Cycloaddition Reaction to Construct Functionalized Hexahydroisoindoles Heerding, D. A.; Takata, D. T.; Kwon, C.; Huffman, W. F.; Samanen J. Tetrahedron Lett. 1998, 39, 6815-6818.

4.7.93. Solid Phase Synthesis of N-Acyl-2-Substituted-Dihydro-4-Pyridone:  Resin Activation/Capture Approach/REACAP Technology Chen, C.; Munoz, B. Tetrahedron Lett. 1998, 39, 6781-6784.

4.7.94. Ration Design and Synthesis of Unsaturated 2,5-Dioxopiperazine Derivatives as Potential Protein Tyrosine Kinase Inhibitors Li. W.-R.; Peng, S.-Z. Tetrahedron Lett. 1998, 39, 7373-7376.

4.7.95. A Practical Solid Phase Synthesis of Quinazoline-2,4-diones Shao, H.; Colucci, M.; Tong, S.; Zhang, H.; Castelhano, A. L. Tetrahedron Lett. 1998, 39, 7235-7238.

4.7.96. Novel Safety-Catch Linker and its Application with a Ugi/De-Boc/Cyclization (UDC) Strategy to access Carboxylic Acids, 1,4-Benodiazepines, Diketopiperazines, Ketopiperazines, and Dihydroquinoxalinones Hulme, C.; Peng, J.; Morton, G.; Salvino, J. M.; Herpin, T.; Labaudiniere, R. Tetrahedron Lett. 1998, 39, 7227-7230.

4.7.97. An Efficient High-Speed Synthetic Route to Amino-Substituted Thiazolidinone Libraries Munson, M.C.; Cook, A. W.; Josey, J. A.; Rao, C. Tetrahedron Lett. 1998, 39, 7223-7226.

4.7.98. Polymer-bound 4-Benzylsulfonyl-1-triphenylphosphoranylidene-2-butanone as a Tool for the Solid-Phase Synthesis of Substituted Piperidin-4-one Derivatives Barco, A.; Benetti, S.; De Risi, C.; Marchetti, P.; Pollini, G. P.; Zanirato, V. Tetrahedron Lett. 1998, 39, 7591-7594.

4.7.99. Combinatorial Modification of 2-Ketopiperazine with Solid Phase C-Alkylation and N-Acylations Zhu, Z.; Mckittrick, B. Tetrahedron Lett. 1998, 39, 7479-7482.

4.7.100. Solid-Phase Synthesis of Substituted 1-Phenyl-2aminomethyl-benzimidazoles and 1-Phenyl-2-thiomethyl-benzimidazoles Tumelty, D.; Schwarz, M. K.; Needels, M. C. Tetrahedron Lett. 1998, 39, 7467-7470.

4.7.101. Polymer-Supported Preparation of Substituted Phenols:  A New Example of Simultaneous Cyclization-Cleavage Reaction on Solid Phase Katritzky, A. R.; Belyakov, S. A.; Fang, Y.; Kiely, J. S. Tetrahedron Lett. 1998, 39, 8051-8054.

4.7.102. Traceless Solid Phase Synthesis of 2,3-Disubstituted Indoles Smith, A. L.; Stevenson, G. I.; Swain, C. J.; Castro, J. L. Tetrahedron Lett. 1998, 39, 8317-8320.

4.7.103. Solid-Phase Synthesis of Pyrroles from Enaminones and Nitroalkenes Trautwein, A. W.; Jung, G. Tetrahedron Lett. 1998, 39, 8263-8266.

4.7.104. Efficient Synthesis of Substituted Oxopiperazines From Amino Acids Mohamed, N.; Bhatt, U.; Just, G. Tetrahedron Lett. 1998, 39, 8213-8216.

4.7.105. Efficient Solid Phase Synthesis of 3,5-Disubstituted Hydantoins Nefzi, A.; Ostresh, J. M.; Giulianotti, M.; Houghten, R. A. Tetrahedron Lett. 1998, 39, 8199-8202.

4.7.106. Solid-Phase Synthesis of a Library of Piperazinediones and Diazepinediones via Kaiser Oxime Resin Smith, R. A.; Bobko, M. A.; Lee, W. Bioorg. Med. Chem. Lett. 1998, 8, 2369-2374.

4.7.107. Novel Safety-Catch Linker and its Application with a Ugi/De-BOC/Cyclization (UDC) Strategy to Access Carboxylic acids, 1,4-Benzodiazepines, Diketopiperazines, Ketopiperazines and Dihydroquinoxalinones Hulme, C.; Peng, J.; Morton, G.; Salvino, J. M.; Herpin, T.; Labaudiniere, R. Tetrahedron Lett. 1998, 39, 7227-7230.

4.7.108.  Heterocyclic Mixture-Based Combinatorial Libraries: Synthesis and Analysis of Composition (3,4-dihydro-2-(1H)-quinolinones) Kiely, J. S.; Pei, Y. Trends in Drug Research II 1998, 29, 147-156.

4.7.109. SN-Ar Cyclization to Form Cyclic Peptidomimetics of beta-Turns Feng, Y.; Wang, Z.; Jin, S.; Burgess, K. J. Am. Chem. Soc. 1998, 120, 10768-10769.

4.7.110. Combinatorial Chemistry of Hydantoins Boeijen, A.; Kruijitzer, J. A. W.; Liskamp, R. M. J. Bioorg. Med. Chem. Lett. 1998, 8, 2375-2380.

4.7.111. Diastereoselective Solid-Phase Synthesis of Novel Hydantoin- and Isoxazoline-Containing Heterocycles Park, K.-H.; Olmstead, M. M.; Kurth, M. J. J. Org. Chem. 1998, 63, 6579-6585.

4.7.112. Stereoselective Synthesis of over Two Million Compounds Having Structual Features Both Reminiscent of Natural Products and Compatible with Miniatureized Cell-Based Assays Tam, D. S.; Foley, M. A.; Shair, M. D.; Schreiber, S. L. J. Am. Chem. Soc. 1998, 120, 8565-8566.

4.7.113. Synthesis of Hydantoins via N,N'-Ureas Derived From Polymer-Bound Amino Acids Bauser, M.; Winter, M.; Valenti, C. A.; Wiesmuller, K.-H.; Jung, G. Molecular Diversity 1998, 3, 257-260.

4.7.114. Lanthanide Triflate-Catalyzed 1,3-Dipolar Cycloaddition Reactions of Polymer-Supported Nitrones with Alkenes for the Preparation of Diverse 2-Isoxazoline Derivatives Tetrahedron Lett. 1998, 39, 9211-9214.

4.7.115. Immobilized Aldehydes and Olefins in the Solid-Phase Synthesis of Tetrahydroquinolines via a Three Component Condensation  Kiselyov, A. S.; Smith, L.; Virgilio, A.; Armstrong, R. Tetrahedron 1998, 54, 7987-7996.

4.7.116. Polymer Bound 3-hydroxy-2-methylidenepropionic Acids.  A Template for Multiple Core Structure Libraries Richter, H.; Walk, T.; Holtzel, A.; Jung, G. J. Org. Chem. 1999, 64, 1362-1365.

4.7.117. Parallel Synthesis of 1,2,3-Thiadiazoles Employing a "Catch and Release" Strategy Hu, Y.; Baudart, S.; Porco, J. A. J. Org. Chem. 1999, 64, 1049-1051.

4.7.118. A Solid Phase Approach to Substituted Pyrimidines and Their Conversion into Condensed Heterocycles for Potential Use in Combinatorial Chemistry Srivastava, S. K.; Haq, W.; Chauhan, P. M. S. Combinatorial Chemistry & High Throughput Screening 1999, 2, 33-37.

4.7.119. Solid-Phase Synthesis of Substituted Benzazepines via Intramolecular Heck Cyclization Bolton, G. L.; Hodges, J. C. J. Combinatorial Chemistry1999, 1, 2, 130-133.

4.7.120. Solid-Phase Synthesis of Cyclic Imides Barn, D. R.; Morphy, J. R. J. Combinatorial Chemistry 1999, 1, 2, 151-156.

4.7.121. Solid-Phase Synthesis of 2,4,6-Trisubstituted Pyridines Chiu, C.; Tang, Z.; Ellingboe, J. W. J. Combinatorial Chemsitry 1999, 1, 1, 73-77.

4.7.122. Solid-phase amino-zinc-enolate cyclization for the synthesis of 3-substituted prolines
Karoyan,  P. ; Triolo, A.; Nannicini, R.; Giannotti, D.; Altamura, M.; Chassaing, G.; Perrotta E. Tetrahedron Letters, 1999, 40, 1, 71-74.

4.7.123. The preparation of 2,4-disubstituted thiazoles on solid support Goff, D.; Fernandez, J. Tetrahedron Letters, 1999, 40, 3, 423-426.

4.7.124.  Solid-Phase Library Synthesis of Triazolopyridazines via [4+2] Cycloadditions Boldi, A. M.; Johnson, C. R.; Eissa, H. O. Tetrahedron Letters, 1999, 40, 4, 619-622.

4.7.125. Solid-Phase Synthesis of 3,5-Disubstituted 2,3-Dihydro-1,5-benzothiazepin-4(5H)-ones Schwarz, M. K.; Tumelty, D.; Gallop, M. A. J. Org. Chem. 1999, 64, 7, 2219-2231.

4.7.126. Solid-Phase Synthesis of 3,4,5-Substituted 1,5-Benzodiazepin-2-ones Lee, J.; Gauthier, D.; Rivero, R. A. J. Org. Chem. 1999, 64, 3060-3065.

4.7.127.  A Novel Solid-Phase Synthesis of Carboxypyrrolinones  Miller, P. C., Owen, T. J., Molyneaux, J. M., Curtis, J. M., Jones, C. R., , J. of Combinatorial Chemistry; 1999, 1, 3, 223-234.

4.7.128.  Solid-Phase Synthesis of Highly Functionalized 2,2'-Bipyridines Tadesse, S., Bhandari, A., Gallop, M. A.,  J. of Combinatorial Chemistry 1999, 1, 3, 184-187.

4.7.129.   Synthesis of 2,4-Disubstituted 2,5-Dihydrofurans and 1-Substituted 1,3-Dihydroisobenzofurans via an Iodine-Magnesium Exchange Reaction Rottlander, M., Knochel, P.,  J. of Combinatorial
Chemistry,1999; 1,3, 181-183.

4.7.130.  Solid-Phase Synthesis of Trisubstituted 2-Imidazolidones and 2-Imidazolidinethiones Nefzi, A., Ostresh, J. M., Giulianotti, M., Houghten, R. A., J. of Combinatorial Chemistry 1999,1, 3, 195-198.

4.7.131.  Solid-phase synthesis of beta-lactams via the Staudinger reaction R. Singh, J. M. Nuss, Tetrahedron Lett. 1999,40, 7, 1249-1252.

4.7.132. Solid-phase synthesis of phenolic steroids: towards combinatorial libraries of estradiol derivatives
M. R. Tremblay, D. Poirier, Tetrahedron Lett. 1999, 40, 7, 1277-1280.

4.7.133. Polymer-supported acylhydrazones. Use in Sc(OTf)3-catalyzed Mannich-type reactions providing an efficient method for the preparation of diverse pyrazolone derivatives S. Kobayashi, T. Furuta, K. Sugita, O. Okitsu, H. Oyamada, Tetrahedron Lett. 1999, 40, 7, 1341-1344.

4.7.134. Solid phase synthesis of 1,3,5-trisubstituted pyridin-2-ones J. A. Linn, S. W. Gerritz, A. L. Handlon, C. E. Hyman, D. Heyer, Tetrahedron Lett. 1999, 40(12), 2227-2230.

4.7.135. Traceless Linkers for Solid-Phase Synthesis - Homo-Diels-Alder and Hetero-Diels-Alder Reactions of O-Quinodimethanes Craig, D.; Robson, M. J., and Shaw, S. J. Synlett 1998; 12, 1381-1383.

4.7.136. Solid-Phase Synthesis of 3-Acyl-2,4-Pyrrolidinediones (3-Acyl Tetramic Acids) via Mild Cyclative Cleavage Romoff, T. T.; Ma, L.; Wang, Y. W., and Campbell, D. A. Synlett 1998; 12, 1341-1342.

4.7.137. Solid-Phase Synthesis of 3H-Quinazolin-4-Ones Based on an Aza Wittig-Mediated Annulation Strategy Villalgordo, J. M.; Obrecht, D.; Chucholowsky, A. Synlett 1998; 12,1405-1407.

4.7.138. Solid-Phase Synthesis of 3-Acyltetramic Acids Weber, L.; Iaiza, P.; Biringer, G., and Barbier, P. Synlett 1998; 10, 1156-1158.

4.7.139. Polymer-Bound 3,5-Cyclohexadiene-1,2-Diols as Core Structures for the Development of Small-Molecule Libraries Wendeborn, S.; Demesmaeker, A.; Brill, W. K. D.  Synlett 1998, 8, 865-868.

4.7.140. A Novel Solution-Phase and Solid-Phase Approach to 2,4,5-Trisubstituted and 2,4,5,6-Tetrasubstituted Pyrimidines and Their Conversion into Condensed Heterocycles Masquelin, T.; Sprenger, D.; Baer, R.; Gerber, F.; Mercadal, Y.  Helv. Chim. Acta. 1998; 81, 4, 646-660.

4.7.l41.  Solution- and Solid-Phase Synthesis of Combinatorial Libraries of Trisubstituted 1,3,5-Triazines  Masquelin, T.; Meunier, N.; Gerber, F., and Rosse, G. Heterocycles 1998; 48(12), :2489-2505.

4.7.142. A Solid-Phase Synthesis of Functionalized 6-Membered, 7-Membered and 8-Membered Azacycles via Olefin Metathesis Pernerstorfer, J.; Schuster, M.; Blechert, S. Synthesis-Stuttgart 1999; (1):138-144.

4.7.143. Stereoselective Solid-Phase Synthesis of -Lactams - A Novel Cyclization/Cleavage Step towards 1-Oxacephams Furman, B.; Thürmer, R.; Kaluza, Z.; Lysek, R.; Voelter, W.; Chmielewski, M. Angew. Chem. Int. Ed. 1999,38(8), 1121-1123.

4.7.144. Solid supported aryl/heteroaryl C-N cross-coupling reactions A. P. Combs, S. Saubern, M. Rafalski, P. Y. S. Lam, Tetrahedron Lett.1999, 40(9), 1623-1626.

4.7.145. Solid support synthesis of 14-membered macrocycles via SNAr methodology on acrylate resin A. S. Kiselyov, S. Eisenberg, Y. Luo, Tetrahedron Lett. 1999, 40(13), 2465-2468.

4.7.146. Novel synthetic routes suitable for constructing benzopyrone combinatorial libraries A. S. Bhat, J. L.Whetstone, R. W. Brueggemeier, Tetrahedron Lett. 1999, 40(13), 2469-2472.

4.7.147. A new 'traceless' solid-phase synthesis strategy: synthesis of a benzimidazole library W. Huang, R. M. Scarborough, Tetrahedron Lett. 1999, 40(14), 2665-2668.

4.7.148. Solid phase synthesis of 2-acyl-3,7,8-substituted-5-oxo-2-azabicyclo-[2.2.2]-octane and triaza analogs: resin activation/capture approach/REACAP technology C. Chen, B. Munoz, Tetrahedron Lett. 1999, 40(18), 3491-3494.

4.7.149. A pseudopeptide platform with side chains addressable for combinatorial applications Rasmussen, P. H.; Rebek, J. Jr. Tetrahedron Lett. 1999, 40(18), 3511-3514.

4.7.150. Novel synthesis of oxindole quinazolines using solid phase multiparallel chemistry L. F. Hennequin, S. Piva-Le Blanc, Tetrahedron Lett. 1999, 40(20), 3881-3884.

4.7.151. A convenient set of bidentate pyridine ligands for combinatorial synthesis F. Wang, A. W. Schwabacher, Tetrahedron Lett. 1999, 40(26), 4779-4782.

4.7.152. Use of the Kaiser Oxime Resin in the Solid-Phase Synthesis of 3-Aminobenzisoxazoles Lepore, S. D.; Wiley, M. R. J. Org. Chem. 1999, 64, 12, 4547-4550.

4.7.153. Solid Phase Diels-Alder Reactions of Amino Acid Derived Trienes Sun, S.; Murray, W. V. J . Org. Chem. 1999, 64, 16, 5941-5945.

4.7.154. Necklace-Coded Polymer-Supported Combinatorial Synthesis of 2-Arylaminobenzimidazoles Smith, J. M.; Gard, J.; Cummings, W.; Kanizsai, A.; Krchnak, V. J. Combinatorial Chemistry 1999, 1, 5, 368-370.

4.7.155. Solid Phase Organic Synthesis of Piperazinone Containing Enkephalin Mimetics:  A Readily Derivatized, Traceless Scaffold Shreder, K.; Zhang, L.; Gleeson, J.-P.; Ericsson, J. A.; Yalamoori, V. V.; Goodman, M. J. Combinatorial Chemistry 1999, 1, 5, 383-387.

4.7.156. Highly efficient and versatile synthesis of libraries of constrained Beta-strand mimetics Ogbu, C.O.;Qabar, M.N.; Boatman, P.D.; Urban, J.; Meara, J.P.; Ferguson, M.D.; Tulinsky, J.; Lum, C.; Babu, S.; Blaskovich, M.A.; Nakanishi, H.; Ruan, F.; Cao, B.; Minarik, R.; Little, T.; Nelson, S.; Nguyen, M.; Gall, A.; Kahn, M.  Bioorg. Med. Chem. Lett. 1998, 8, 2321-2326.

4.7.157.  Cyclisation/cleavage of macrocycles by ring-closing metathesis on solid support-conformational studies J. Pernerstorfer, M. Schuster, S. Blechert Chem. Commun. 1997, 1949-1950.

4.7.158. Stereoselective Solid-Phase Synthesis of a Triaza Tricyclic Ring System: A New Chemotype for Lead Discovery G. Peng, A. Sohn, and M. A. Gallop J. Org. Chem.; 1999; 64(22), 8342-8349

4.7.159. A new and simple "lego" system for the synthesis of branched oligopyridines Pabst, G.R.; Schmid, K.; Sauer, J. Tetrahedron Lett.1998,39, 6691-6694.

4.7.160. Solid phase synthesis of highly substituted 2,4-dioxopiperidines W. Chai, W. V. Murray Tetrahedron Lett., 1999, 40, 7185-7188.

4.7.161. Solid-phase intermolecular radical reactions. Part 1: sulfonyl radical addition to isolated alkenes and alkynes S. Caddick, D. Hamza, S. N. Wadman Tetrahedron Lett., 1999, 40, 7285.

4.7.162. Solid phase synthesis of quinolones S. K. Srivastava, W. Haq, P. K. Murthy, P. M. S. Chauhan Bioorg. Med. Chem. Lett.1999,9 (14), 1885-1888.

4.7.163. Oxadiazole synthesis on solid supports G.-B. Liang, X. Qian Bioorg. Med. Chem. Lett. 1999, 9(14), 2101-2104.

4.7.164. Solid-Phase Synthesis of Substituted 4-Acyl-1,2,3,4-tetrahydroquinoxalin-2-ones Zaragoza, F.,Stephensen, H. J. Org. Chem.; 1999; 64(7); 2555-2557.

4.7.165. A Facile Method for the Solution and Solid-Phase Synthesis of Substituted [3.3.1] Bicycles Nicolaou, K. C., Pfefferkorn, J. A., Cao, G.-Q., Kim, S., Kessabi, J., Org. Lett., 1999; 1(5); 807-810.

4.7.166. Practical synthesis of tetrasubstituted thiophenes for use in compound libraries B. P. McKibben, C. H. Cartwright, A. L. Castelhano Tetrahedron Lett. 1999, 40(30), 5471-5474.

4.7.167. A solid-phase equivalent of van Leusen's TosMIC, and its application in oxazole synthesis B. A. Kulkarni, A. Ganesan Tetrahedron Lett. 1999, 40(30), 5633-5636.

4.7.168. Solid phase synthesis of tetrahydropyrazine-2-ones by intramolecular Mitsunobu reactions P.-P. Kung, E. Swayze Tetrahedron Lett. 1999, 40(31), 5651-5654.

4.7.169. Solid-phase synthesis of N-hydroxyindoles and benzo[c]isoxazoles by C-arylation of substituted acetontriles and 1,3-dicarbonyl compounds with polystyrene-bound aryl fluorides H. Stephensen, F. Zaragoza Tetrahedron Lett. 1999, 40(31), 5799-5802.

4.7.170. An uncatalyzed cyclo-elimination process for the release of N3-alkylated hydantoins from solid-phase: synthesis of novel isoxazoloimidazolidinediones K.-H. Park, M. J. Kurth Tetrahedron Lett. 1999, 40(32), 5841-5844.

4.7.171. A new acetal resin valuable for the solid-phase synthesis of 1-oxacephams via a cyclization/cleavage step B. Furman, R. Thurmer, Z. Kaluza, W. Voelter, M. Chmielewski Tetrahedron Lett. 1999,40(32), 5909-5912.

4.7.172. Synthesis of azepane scaffolds on solid support for combinatorial chemistry L. Gauzy, Y. Le Merrer, J.-C. Depezay, F. Clerc, S. Mignani Tetrahedron Lett. 1999, 40(33), 6005-6008.

4.7.173. Solid-phase synthesis of substituted benzimidazoles D. Tumelty, M. K. Schwarz, K. Cao, M. C. Needels Tetrahedron Lett.1999,40(34), 6185-6188.

4.7.174. Solid-phase synthesis of substituted cinnolines by a Richter type cleavage protocol S. Brase, S. Dahmen, J. Heuts Tetrahedron Lett. 1999, 40(34), 6201-6204.

4.7.175. High-throughput combinatorial synthesis of substituted benzimidazolones P.-C. Pan, C.-M. Sun Tetrahedron Lett. 1999, 40(35), 6443-6446.

4.7.176. Solid phase synthesis of aziridine 2-carboxylates S. N. Filigheddu, S. Masala, M. Taddei Tetrahedron Lett. 1999,40(35), 6503-6506.

4.7.177. A new solid-phase linker for Suzuki coupling with concomitant macrocyclization: synthesis of beta-turn mimics W. Li, K. Burgess Tetrahedron Lett. 1999, 40(36), 6527-6530.

4.7.178. Solid phase synthesis of 1,3,5-trisubstituted pyridin-2-ones J. A. Linn, S. W. Gerritz, A. L. Handlon, C. E. Hyman, D. Heyer, Tetrahedron Lett. 1999, 40(12), 2227-2230.

4.7.179.  A convenient Procedure for the solution Phase Preparation of 2-Aminothiazole Combinatorial Libraries Bailey, N., Dean, A. W.; Judd, D. B.; Middlemiss, D.; Storer, R.; Watson, S. P. Bioorg. Med. Chem. Lett. 1996, 6, 1409-1414.

4.7.180. Solid phase hydantoin synthesis: An efficient and direct conversion of Fmoc-protected dipeptides to hydantoins Chong, P. Y. ; Petillo, P. A. Tetrahedron Lett. 1999, 40(13), 2493-2496.

4.7.181. Solid phase synthesis  of N-arylazoindoles Khound, S.; Das, P. J. Tetrahedron  1997, 53(28), 9749-9754.

4.7.182. The "One-Bead-One-Compound" Combinatorial Library Method Lam. K. S.; Lebl, M.; Krcknak, V. Chemical Reviews 1997, 97(2), 411-448.

4.7.183. Solution-Phase and Solid-Phase Synthesis of Novel Hydantoin and Isoxazoline-Containing Heterocycles Park, K. H.; Abbate, E.; Najdi, S.; Olmstead, M. M., and Kurth, M. J Chem. Comm. 1998; (16), 1679-1680.

4.7.184. Synthesis of small and medium sized 2,2-disubstituted lactams via the "intramolecular" three component Ugi reaction Harriman, G.C.B. Tetrahedron Lett. 1997, 38, 5591-5594.

4.7.185. Solid phase applications of Dde and the analogue Nde: Synthesis of trypanothione disulphide Kellam, B., Bycroft, B.W., Chhabra, S.R. Tetrahedron Lett. 1997, 38, 4849-4852.

4.7.186. Facile preparation of 2,6-disubstituted purines using solid-phase chemistry Nugiel, D.A., & Cornelius, L.A.M. J. Org. Chem. 1997, 62, 201-203.

4.7.187. Combinatorial synthesis of 2-thioxo-4-dihydropyrimidinones Sim, M.M., Lee, C.L., Ganesan, A. J. Org. Chem. 1997, 62, 9358-9360.

4.7.188. Selective solid phase synthesis of ureas and hydantoins from common phenyl carbamate intermediates Xiao, X.Y., Ngu, K., Chao, C., & Patel, D.V. J. Org. Chem. 1997, 62, 6968-6973.

4.7.189. Solid-phase synthesis of isoxazoles and isoxazolines: En route to a new class of ionophores Kantorowski, E.J., & Kurth, M.J. J. Org. Chem. 1997, 62, 6797-6803.

4.7.190. Base-promoted solid-phase synthesis of substituted hydantoins and thiohydantoins Matthews, J., & Rivero, R.A. J. Org. Chem. 1997, 62, 6090-6092.

4.7.191. Utility of complementary molecular reactivity and molecular recognition (CMR/R) technology and polymer-supported reagents in the solution-phase synthesis of heterocyclic carboxamides Parlow, J.J., Mischke, D.A., & Woodard, S.S. J. Org. Chem. 1997, 62, 5908-5919.

4.7.192. Polymer-supported synthesis of diverse perhydro-1,4-diazepine-2,5-diones Krchnak, V., Weichsel, A.S. Tetrahedron Lett. 1997, 38, 7299-7302.

4.7.193. Solid-phase synthesis of benzopiperazinones Morales, G.A., Corbett, J.W., DeGrado, W.F. J. Org. Chem. 1998, 63, 1172-1177.

4.7.194. A novel cleavage technique to generate small molecule compounds and libraries via a two-resin system Ouyang, X., Armstrong, R.W., & Murphy, M.M. J. Org. Chem. 1998, 63, 1027-1032.

4.7.195. Isoxazolinoisoquinoline heterocycles via solid-phase Reissert and Suzuki reactions Lorsbach, B.A., Bagdanoff, J.T., Miller, R.B., Kurth, M.J. J. Org. Chem. 1998, 63, 2244-2250.

4.7.196. Ketenes in soluble polymer bound synthesis: Preparation of succinamides and 4-pyridones Far, A.R., Tidwell, T.T. J. Org. Chem. 1998, 63, 8636-8637.

4.7.197. Solid-phase synthesis of trisubstituted bicyclic guanidines via cyclization of reduced N-acylated dipeptides. Ostresh, J.M., Schoner, C.C., Hamashin, V.T., Nefzi, A., Meyer, J.P., Houghten, R.A. J. Org. Chem. 1998, 63, 8622-8623.

4.7.198. Carbohydrates as multifunctional chiral scaffolds in combinatorial synthesis Wunberg, T.; Kallus, C.; Opatz, T.; Henke, S.; Schmidt, W.; Kunz, H. Angew. Chem. Int. Ed. 1998, 37, 2503-2505.

4.7.199. A New Heterocyclic Multicomponent Reaction for the Combinatorial Synthesis of Fused 3-Aminoimidazoles Bienayme, H.; Bouzid, K. Angew. Chem. Int. Ed. 1998; 37(16) 2234-2237.

4.7.200. Combinatorial Solid-Phase Synthesis of Structurally Complex Thiazolylhydantoines . Stadlwieser, J.; Ellmerermuller, E. P.; Tako, A.; Maslouh, N.; Bannwarth, W. Angew. Chem. Int. Ed. 1998; 37(10) 1402-1404.

4.7.201. An Enzyme-Labile Linker Group for Organic Syntheses on Solid Supports Sauerbrei, B.; Jungmann, V.; Waldmann, H. Angew. Chem. Int. Ed. 1998; 37(8) 1143-1146.

4.7.202. Virtual combinatorial libraries: Dynamic generation of molecular and supramolecular diversity by self-assembly Huc, I.; Lehn, J.M. Proc. Natl. Acad. Sci. USA 1997, 94, 2106-2110.

4.7.203. MCR 6: Chiral 2,6-Piperazindiones via Ugi Reactions with alpha-Amino Acids, Carbonyl Compounds, Isocyanides and Alcohols Ugi, I.; Horl, W.; Schmid, T.; Hanusch-Kompa, C.; Herdtweck, E. Heterocycles 1998,47 (2), 965-975.

4.7.204. A Novel Solution- and Solid-Phase Approach to 2,4,5-Tri and 2,4,5,6-Tetrasubstituted Pyrimidines and their Conversion into Condensed Heterocycles Masquelin, T.; Sprenger, D.; Baer, R.; Gerber, F.; Mercadal, Y. Helv. Chim. Acta. 1998, 81, 646-660.

4.7.205. MCR V. The Seven Component Reaction Domling, A.; Herdtweck, E.; Ugi, I. Acta Chem. Scand. 1998, 52, 107-113.

4.7.206. New cleavage approaches to combinatorial synthesis of homoserine lactones Ko, D.H.; Kim, D.J.; Lyu, C.S.; Min, I.K.; Moon, H.S. Tetrahedron Lett. 1998, 39, 297-300.

4.7.207. Natural products analogs as scaffolds for supramolecular and combinatorial chemistry Mink, D.; Mecozzi, S.; Rebek, J.Jr. Tetrahedron Lett. 1998, 39, 5709-5712.

4.7.208. Solid-phase synthesis of N-acyl-N'-carbamoylguanidines Lin, P.; Ganesan, A. Tetrahedron Lett. 1998, 39, 9789-9792.

4.7.209. Fast and efficient synthesis of substituted dibenz[b,f]oxazocines on solid support Ouyang, X.; Kiselyov, A. S. Tetrahedron 1999, 55(28), 8295 -8302.

4.7.210. A Metathetical Cycloaddition-Cycloreversion Approach to the Formation of Furan Scaffold Libraries Whitehouse, D.L., Nelson, K.H., Savinov, S.N., Lowe, R.S., Austin, D.J. Bioorg. Med. Chem. 1998, 6, 1273-1282.

4.7.211. Solid phase organic synthesis of polyamine derivatives and initial biological evaluation of their antitumoral activity Tomasi, S.; Le Roch, M.; Renault, J.; Corbel, J.-C.; Uriac, P.; Carboni, B.; Moncoq, D.; Martin, B.; Delcros, J.-G. Bioorg. Med. Chem.Lett. 1998, 8, 635-640.

4.7.212. Discovery of a New Cyclooxygenase-2 Lead Compound Through 3-D Database Searching and Combinatorial Chemistry Stewart, K. D.; Loren, S.; Frey, L.; Otis, E.; Klinghofer, V.; Hulkower, K. I. Bioorg. Med. Chem. Lett. 1998, 8, 529-534.

4.7.213. Solid phase synthesis of structurally diverse pyrimido[4,5-d]pyrimidines for the potential use in combinatorial chemistry Srivastava, S. K.; Haq, W.; Chauhan, P. M. S Bioorg. Med. Chem. Lett. 1999, 9, 965-966.

4.7.214. Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: Identification of avb3 antagonists lead compounds Rockwell, A. L.; Rafalski, M.; Pitts, W. J.; Batt, D. G.; Petraitis, J. J.; DeGrado, W. F.; Mousa, S.; Jadhav, P. K. S Bioorg. Med. Chem. Lett. 1999, 9, 937-942.

4.7.215. Solid-Phase Synthesis of Benzisothiazolones as Serine-Protease Inhibitors Yu, K. L.; Civiello, R.; Roberts, D. G. M.; Seiler, S. M.; Meanwell, N. A. S Bioorg. Med. Chem. Lett. 1999, 9, 663-666.

4.7.216. Liquid-Phase Combinatorial Synthesis of Benzylpiperazines Bioorg. Med. Chem. Lett. 1999, 9 (4) 519-522.

4.7.217. Combinatorial synthesis of indolizines on solid support Goff, D. A. Tetrahedron Lett. 1999, 40(50), 8741.

4.7.218. An approach to combinatorial library generation of galactofuranose mimics as potential inhibitors of mycobacterial cell wall biosynthesis: Synthesis of a peptidomimetic of uridine 5'-diphosphogalacto-furanose (UDP-Galf) Lee, R. E.; Smith, M. D.; Pickering, L.; Fleet, G. W. J. Tetrahedron Lett. 1999, 40(49), 8689-8692.

4.7.219. Synthesis of oxadiazoles on solid support Hébert, N.; Hannah, A. L.; Sutton, S. C. Tetrahedron Lett. 1999, 40(49), 8547-8550.

4.7.220. Solid-phase synthesis of heterocycles via palladium-catalyzed annulation Wang, Y.; Huang, T.-N. Tetrahedron Lett. 1998, 39, 9605-9608.

4.7.221. Synthesis of acetoxyamides and acetates by zinc bromide assisted cleavage of Merrifield resin-bound ethers Li, W.-R.; Yo, Y.-C.Tetrahedron Lett. 1999, 40(51), 9085-9089.

4.7.222. A decarboxylative traceless linker approach for the solid phase synthesis of quinazolines Cobb, J. M.; Fiorini, M. T.; Goddard, C. R.; Theoclitou, M.-E.; Abell. C. Tetrahedron Lett. 1999, 40(5), 1045 -1048.

4.7.223. Solid-phase synthesis of N-hydroxyindoles and benzo[c]isoxazoles by C-arylation of substituted acetontriles and 1,3-dicarbonyl compounds with polystyrene-bound aryl fluorides Stephensen, H.; Zaragoza, F. Tetrahedron Lett. 1999, 40(31), 5799-5802.

4.7.224. Solid phase synthesis of tetrahydropyrazine-2-ones by intramolecular Mitsunobu reactions Kung, P.-P.; Swayze, E. Tetrahedron Lett. 1999, 40(31), 5651-5654.

4.7.225. Solution-phase parallel oxazole synthesis with TosMIC Kulkarni, B. A.; Ganesan, A. Tetrahedron Lett. 1999, 40(30), 5637-5638.

4.7.226. A solid-phase equivalent of van Leusen's TosMIC, and its application in oxazole synthesis Kulkarni, B. A.; Ganesan, A. Tetrahedron Lett. 1999, 40(30), 5633-5636.

4.7.227. Practical synthesis of tetrasubstituted thiophenes for use in compound libraries McKibben, B. P.; Cartwright, C. H.; Castelhano, A. L. Tetrahedron Lett. 1999, 40(30), 5471-5474.

4.7.228. Liquid-Phase Synthesis of 2-(alkylthio) benzimidazoles Yeh, C.-M.; Sun, C.-M. Tetrahedron Lett. 1999, 40, 7247-7250.

4.7.229. Characterization of Spatially Addressable Libraries: Stereoisomer Analysis of Tetrahydro-b -carbolines as an Example Cheng, C. C.; Chu, Y.-H. Journal of Combinatorial Chemistry 1999, 1(6), 461-466.

4.7.230. Solid support synthesis of polysubstituted tetrahydroquinolines via three-component condensation catalyzed by Yb(OTf)3 Kiselyov, A. S.; Smith, L. II, Armstrong, R. W. Tetrahedron 1998, 54(20), 5089-5096. 

4.7.231. Parallel synthesis of polysubstituted tetrahydroquinolines Baudelle, R.; Melnyk, P.; Deprez, B.; Tartar, A. Tetrahedron 1998, 54(16) 4125-4140.

4.7.232. Automated parallel synthesis of chalcone-based screening libraries Powers, D. G.; Casebier, D. S.; Fokas, D.; Ryan, W. J.; Troth, J. R.; Coffen, D. L. Tetrahedron 1998, 54(16) 4085-4096.

4.8. Targetted Libraries Prepared on Solid Support

4.8.1. Libraries of Angiotensin Converting Enzyme Inhibitors: Solid-Phase Synthesis and Affinity Selection Blackburn, C.; Pingali, A.; Kehoe, T.; Herman, L. W.; Wang, H.; Kates, S. A. Bioorg. Med. Chem. Lett. 1997, 7, 823-826.

4.8.2. Structure-Based Design and Combinatorial Chemistry Yield Low Nanomolar Inhibitors of Cathepsin D Kick, E. K.; Roe, D. C.; Skillman, A. G.; Liu, G.; Ewing, T. J. A.; Sun, Y.; Kuntz, I. D.; Ellman, J. A. Chem. Biol. 1997, 4, 297-307.

4.8.3. A Combinatorial Approach for Determining Protease Specificities: Application to Interleukin-1beta Converting Enzyme (ICE) Rano, T. A.; Timkey, T.; Peterson, E. P.; Rotonda, J.; Nicholson, D. W.; Becker, J. W.; Chapman, K. T.; Thornberry, N. A. Chem. Biol. 1997, 4, 149-155.

4.8.4. Solid-Phase Synthesis of a Selective alpha(v)-beta(3) Integrin Antagonist Library Corbett, J. W.; Graciani, N., R.; Mousa, S. A.; DeGrado, W. F. Bioorg. Med. Chem. Lett. 1997, 7, 1371-1376.

4.8.5. Solid-Phase Synthesis of Hydrid Thiazolidinedione-Fatty Acid PPAR-gamma Ligands Tomkinson, N. C. O.; Sefler, A. M.; Plunkt, K. D.; Blanchard, S. G.; Parks, D. J.; Willson, T. M. Bioorg. Med. Chem. Lett. 1997, 7, 2491-2496.

4.8.6. Solid Phase Synthesis of Olefin and Hydroxyethylene Peptidomimetics Rotella, D. P. J. Am. Chem. Soc. 1996, 118, 12246-12247.

4.8.7. Combinatorial Chemical Approaches as an Efficient Tool for Discovering GPIIb/IIIa Antagonists Hayashi, Y.; Harada, T.; Katada, J.; Uno, I. Drugs of the Future 1997, 22, 12, 1367-1373.

4.8.8. Identification of Peroxisome Proliferator-Activated Receptor Ligands from a Biased Chemical Library Brown, P. J. et al Chem. Biol. 1997, 4, 909-918.

4.8.9. Solid Phase Synthesis of Benzylamine-Derived Sulfonamide Library Kim, S. W.; Hong, C. Y.; Koh, J. S.; Lee, E. J.; Lee, K. Molecular Diversity 1998, 3, 133-136.

4.8.10. Solid Phase Synthesis of 2,6-Disubstituted-4(3H)-pyrimidinones Targeting HIV-1 Reverse Transcription Nizi, E.; Botta, M.; Corelli, F.; Manetti, F.; Messina, F.; Maga, G. Tetrahedron Lett. 1998, 39, 3307-3310.

4.8.11. Carbohydrate-Based Combinatorial Libraries Sofia, M. J. Molecular Diversity 1998, 3, 75-94.

4.8.12. A Combinatorial Synthesis of Tyrophostins via the "Directed Sorting" Method Shi, S.; Xiao, X-y.; Czarnik, A. W. Biotechnology and Bioengineering (Combinatorial Chemistry) 1998, 61, 1, 7-12.

4.8.13. Efficient Synthesis of Diverse Monosaccharide Derivatives in the Solid Phase Kobayashi, S.; Wakabayashi, T.; Yasuda, M. J. Org. Chem. 1998, 63, 4868-4869.

4.8.14. Serine Proteases-Directed Small Molecule Probe Libraries Dhanoa, D. S. et al. Med. Chem. Res. 1998, 8:4/5, 187-205.

4.8.15. Carbohydrate-Based Combinatorial Libraries Sofia, M. J. Molecular Diversity 1998, 3, 75-94.

4.8.16. Two-Dimensional Parallel Array Technology as a New Approach to Automated Combiantorial Solid-Phase Organic Synthesis (hydroxamic acids with antibacterial activity) Brennan, T.; et al. Biotechnology and Bioengineering (Combinatorial Chemistry) 1998, 61, 1, 33-46.

4.8.17. Solid and Solution Phase Synthesis and Biological Evaluation of Combinatorial Sarcodictyin Libraries Nicolaou, K. C.; Winssinger, N.; Vourloumis, D.; Ohshima, T.; Kim, S.; Pfefferkorn, J.; Xu, J.-Y.; Li, T. J. Am. Chem. Soc. 1998, 120, 10814-10826.

4.8.18. Solid-Phase Synthesis of Oligosaccharides and Glycoconjugates by the Glycal Assembly Method:  A Five Year Retrospective Seeberger, P. H.; Danishefsky, S. J. Acc. Chem. Res. 1998, 31, 685-695.

4.8.19. A Library Approach to the Discovery of Small Molecules That Recognize RNA:  Use of a 1,3-Hydroxyamine Motif as Core Wong, C-. H.; Hendrix, M.; Manning, D. D.; Rosenbohm, C.; Greenberg, W. A. J. Am. Chem. Soc. 1998, 120, 8319-8327.

4.8.20. General Solid-Phase Synthesis Approach To Prepare Mechanism-Based Aspartyl Protease Inhibitor Libraries.  Identification of Potent Cathepsin D Inhibitors Lee, C. E.; Kick, E. K.; Ellman, J. A. J. Am. Chem. Soc. 1998, 120, 9735-9747.

4.8.21. Designed Epothilones:  Combinatorial Synthesis, Tubulin Assembly Properties, and Cytotoxic Action against Taxol-Resistant Tumor Cells Nicolaou, K. C. et al Angew. Chem. Int. Ed. Engl. 1997, 36, 19, 2097-2103.

4.8.22. Rapid Identification of Subtype-Selective Agonists of the Somatostatin Receptor Through Combinatorial Chemistry Rohrer, S. P. et al Science, 1998, 282, 737-740.

4.8.23. Combinatorial Synthesis and Screening of a Chemical Library of 1,4-Dihydropyridine Calcium Channel Blockers Gordeev, M. F.; Patel, D. V.; England, B. P.; Jonnalagadda, S.; Combs, J. D.; Gordon, E. M. Bioorg. Med. Chem. 1998, 6, 883-889.

4.8.24. Synthesis and Evaluation of Paclitaxel C7 Derivatives: Solution Phase Synthesis of Combinatorial Libraries Bhat, L.; Liu, Y.; Victory, S. F.; Himes, R. H.; Georg, G. I. Bioorg. Med. Chem. Lett. 1998, 8,3181-3186.

4.8.25. The Solid Phase Synthesis of a Series of Tri-Substituted Hydantoin Ligands for the Somatostatin SST5 Receptor Scicinski, J. J.; Barker, M. D.; Murray, P. J.; Jarvie, E. M. Bioorg. Med. Chem. Lett. 1998, 8, 3609-3614.

4.8.26.  Solid-Phase Synthesis of a Combinatorial Array of 1,3-Bis(acylamino)-2-butanones, Inhibitors of the Cysteine Proteases Cathepsins K and L Yamashita, D. S., Dong, X., Oh, H.-J., Brook, C. S., Tomaszek, T. A., Szewczuk, L., Tew, D. G., Veber, D. F., J. of Combinatorial Chemistry 1999; 1, 3, 207-215.

4.8.27. Combinatorial Synthesis and Modification of Functional Porphyrin Libraries:  Identification of New, Amphipathic Motifs for Biomolecule Binding Drain, C. M.; Gong, X.; Ruta, V.; Soll, C. E.; Chicoineau, P. F. J. of Combinatorial Chemistry 1999; 1, 4, 286-290.

4.8.28. Solid-Phase Synthesis of Novel Inhibitors of Farnesyl Transferase  Barber, A. M.; Hardcastle, I. R.; Rowlands, M. G.; Nutley, B. P.; Marriott, J. H., and Jarman, M.  Bioorg. Med. Chem. Lett. 1999;9(4):623-626.

4.8.29. Solid-Phase Synthesis of Levoglucosan Derivatives Brill, W. K. D.; Demesmaeker, A., and Wendeborn, S.  Synlett 1998;10, 1085-1090.

4.8.30. Solid and solution phase synthesis of -keto amides via azetidinone ring-opening: application to the synthesis of poststatin S.-K. Khim, J. M. Nuss Tetrahedron Lett. 1999, 40(10), 1827-1830.

4.8.31. Solid-phase synthesis of potential aspartic acid protease inhibitors containing a hydroxyethylamine isostere J. Zhou, A. Termin, M. Wayland, C. M. Tarby, Tetrahedron Lett. 1999, 40(14), 2729-2732.

4.8.32. Stereospecific Solution- and Solid-Phase Glycosylations.  Synthesis of beta-Linked Saccharides and Construction of Disaccharide Libraries Using Phenylsulfenyl 2-Deoxy-2-Trifluoroacetamido Glycopyranosides as Glycosyl Donors Silva, D. J.; Wang, H.; Allanson, N. M.; Jain, R. K.; Sofia, M. J. J. Org. Chem. 1999, 64, 16, 5926-5929.

4.8.33. Solid-Phase SN2 Macrocyclization Reactions to Form beta-Turn Mimics Feng, Y.; Pattarawarapan, M.; Wang, Z.; Burgess, K. Org. Lett., 1999, 1, 1, 121-124.

4.8.34. Identification of a Potent Heterocyclic Ligand To Somatostatin Receptor Subtype 5 by the Synthesis and Screening of beta-Turn Mimetic Libraries Souers, A. J.; Virgilio, A. A.; Rosenquist, A.; Fenuik, W.; Ellman, J. A. J. Am. Chem. Soc. 1999, 121, 1817-1825.

4.8.35. A Combinatorial Approach Toward the Discovery of Non-Peptide, Subtype-Seletive Somatostatin Receptor Ligands Berk, S. C.; Rohrer, S. P.; Degrado, S. J.; Birzin, E. T.; Mosley, R. T.; Hutchins, S. M.; Pasternak, A.; Schaeffer, J. M.; Underwood, D. J.; Chapman, K. T. J. Combinatorial Chemistry 1999, 1, 5, 388-396.

4.8.36. Amidoglycosylation of Polymer-Bound Glycals: A Complete Solid-Phase Synthesis of the Oligosaccharide Domain of the Lewis Blood Group Determinant C. Zheng, P. H. Seeberger, S. J. Danishefsky Angew.Chem. Int.Ed.1998,37, 786-789.

4.8.37. Solid-Phase Supported Synthesis of the Branched Pentasaccharide Moiety That Occurs in Most Complex Type N-Glycan Chains J. Rademann, A. Geyer, R. R. Schmidt Angew.Chem.Int.Ed. 1998, 37, 1241-1245.

4.8.38. Solid-Phase Synthesis of Oligosaccharides: Construction of a Dodecasaccharide K. C. Nicolaou, N. Watanabe, J. Li, J. Pastor, N. Winssinger  Angew.Chem.Int.Ed. 1998, 37, 1559-1561.

4.8.39. Parallel Synthesis of Sialyl Lewis X Mimetics on a Solid Phase: Access to a Library of Fucopeptides T. F. J. Lampe, G. Weitz-Schmidt, C.-H. Wong  Angew.Chem.Int.Ed. 1998, 37, 1707-1711.

4.8.40. A Two-Directional Approach for the Solid-Phase Synthesis of Trisaccharide Libraries T. Zhu, G.-J. Boons  Angew.Chem. Int.Ed. 1998, 37, 1898-1900.

4.8.41. Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors Baker, C.T.; Salituro, F.G.; Court, J.J.; Deininger, D.D.; Kim, E.E.; Li, B.; Novak, P.M.; Rao, B.G.; Pazhanisamy, S.; Schairer, W.C.; Tung, R.D.  Bioorg. Med. Chem. Lett. 1998, 8, 3631-3636.

4.8.42. A general and highly efficient solid phase synthesis of oligosaccharides. Total synthesis of a heptasaccharide phytoalexin elicitor (HPE) Nicolaou, K.C., Winssinger, N., Pastor, J., & DeRoose, F. J. Amer. Chem. Soc.,1997, 119, 449-450.

4.8.43. Intramolecular Aglycon Delivery on Polymer Support: Gatekeeper Monitored Glycosylation Y. Ito, T. Ogawa, J.Am.Chem. Soc. 1997, 119, 5562-5566.

4.8.44. Solid-phase synthesis of artificial beta-sheets Holmes, D.L., Smith, E.M., Nowick, J.S. J. Amer. Chem. Soc. 1997, 119, 7665-7669.

4.8.45. Dihydropyrancarboxamides related to Zanamivir: a new series of inhibitors of influenza  virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4H-pyran-6-carboxamides Smith, P.W.; Sollis, S.L.; Howes, P.D.; Cherry, P.C.; Starkey, I.D.; Cobley, K.N.; Weston, H.; Scicinski, J.; Merritt, A.; Whittington, A.; Wyatt, P.; Taylor, N.; Green, D.; Bethell, R.; Madar, S.; Fenton, R.J.; Morley, P.J.; Pateman, T.; Beresford, A. J. Med. Chem. 1998, 41, 787-797.

4.8.46. Identification of an opioid k receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine Thomas, J.B.; Fall, M.J.; Cooper, J.B.; Rothman, R.B.; Mascarella, S.W.; Xu, H.; Partilla, J.S.; Dersch, C.M.; McCullough, K.B.; Cantrell, B.E.; Zimmermann, D.M.; Carroll, F.I.  J. Med. Chem. 1998,41, 5188-5197.

4.8.47. Repetitive Solid Phase Glycosylation on an Alkyl Thiol Polymer Leading to Sugar Oligomers Containing 1,2-trans- and 1,2-cis-Glycosidic Linkages J. Rademann, R. R. Schmidt,  J.Org.Chem. 1997, 62, 3650-3653.

4.8.48. Polymer-supported oligosaccharides via N-pentenyl glycosides: Methodology for a carbohydrate library  Rodebaugh, R., Joshi, S., Fraser-Reid, B., Geysen, H.M.  J. Org. Chem. 1997, 62, 5660-5661.

4.8.49. Solid Support Oligosaccharide Synthesis: Construction of beta-Linked Oligosaccharides by Coupling of Glycal Derived Thioethyl Glycosyl Donors Zheng, C., Seeberger, P.H., Danishefsky, S.J. J.Org.Chem.1998, 63, 1126-1130.

4.8.50. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors Gray, N.S.; Wodicka, L.; Thunnissen, A.-M.W.H.; Norman, T.C.; Kwon, S.; Espinoza, F.H.; Morgan, D.O.; Barnes, G.; LeClerc, S.; Meijer, L.; Kim, S.-H.; Lockhart, D.J.; Schultz, P.G. Science, 1998, 281, 533-538.

4.8.51. Solvent effect in glycosylation reaction on polymer support S.Manabe, Y.Ito, T.Ogawa Synlett, 1998, 628-630.

4.8.52. Rapid parallel synthesis applied to the optimization of a series of potent nonpeptide neuropeptide Y-1 receptor antagonists M. G. Siegel, M. O. Chaney, R. F. Bruns, M. P. Clay, D. A. Schober, A. M. Van Abbema, D. W. Johnson, B. E. Cantrell, P. J. Hahn, D. C. Hunden, D. R. Gehlert, H. Zarrinmayeh, P. L. Ornstein, D. M. Zimmerman, G. A. Koppel Tetrahedron, 1999,55, 11619.

4.8.53. Solid phase chemistry approach to the SAR development of a novel class of active site-directed thrombin inhibitors M. G. Johnson, D. D. Bronson, J. E. Gillespie, D. S. Gifford-Moore, K. Kalter, M. P. Lynch, J. R. McCowan, C. C. Redick, D. J. Sall, G. F. Smith, R. J. Foglesong Tetrahedron, 1999, 55, 11641

4.8.54. Solid phase parallel synthesis of highly substituted thiophene derivatives and identification of novel phosphodiesterase-4 (PDE-4) inhibitors Y. Han, A. Giroux, C. Lépine, F. Laliberté, Z. Huang, H. Perrier, C. I. Bayly, R. N. Young  Tetrahedron, 1999,55, 11669.

4.8.55. Fragment condensation of solid-phase in the synthesis of an amphiphilic glycopeptide from the hemophilic recognition domain of epithelial cadherin 1  J. Habermann, H. Kunz Tetrahedron Lett. 1998, 39, 4797-4800.

4.8.56. Combinatorial discovery process yields antimicrobial peptoids S. Ng, B. Goodson, A. Ehrhardt, W. H. Moos, M. Siani, J. Winter Bioorg. Med. Chem. 1999, 7(9), 1781.

4.8.57. Combinatorial Library Approach for the Identification of Synthetic Receptors Targeting Vancomycin-Resistant Bacteria Xu, R.,Greiveldinger, G.,Marenus, L. E.,Cooper, A.,Ellman, J. A., J. Am. Chem. Soc.; 1999;121(20); 4898-4899.

4.8.58. An Efficient Solid-Phase Synthesis of the Vitamin D3 System Doi, T., Hijikuro, I., Takahashi, T., J. Am. Chem. Soc.; 1999; 121(28); 6749-6750.

4.8.59. Identification of Highly Selective Inhibitors of Collagenase-1 from Combinatorial Libraries of Diketopiperazines Szardenings, A. K.,Antonenko, V.,Campbell, D. A.,DeFrancisco, N.,Ida, S.,Shi, L.,Sharkov, N.,Tien, D.,Wang, Y.,Navre, M.  J. Med. Chem.; 1999; 42(8); 1348-1357.

4.8.60. Discovery of Novel Disaccharide Antibacterial Agents Using a Combinatorial Library Approach Sofia, M. J., Allanson, N., Hatzenbuhler, N. T., Jain, R., Kakarla, R., Kogan, N., Liang, R., Liu, D., Silva, D. J., Wang, H., Gange, D., Anderson, J., Chen, A., Chi, F., Dulina, R., Huang, B., Kamau, M., Wang, C., Baizman, E., Branstrom, A., Bristol, N., J. Med. Chem.; 1999; 42(17); 3193-3198.

4.8.61. A Combinatorial Approach to the Identification of Dipeptide Aldehyde Inhibitors of -Amyloid Production Higaki, J. N., Chakravarty, S., Bryant, C. M., Cowart, L. R., Harden, P., Scardina, J. M., Mavunkel, B., Luedtke, G. R., Cordell, B., J. Med. Chem.; 1999; 42(19); 3889-3898.

4.8.62. Combinatorial Library of Serine and Cysteine Protease Inhibitors That Interact with Both the S and S' Binding Sites Abato, P., Conroy, J. L., Seto, C. T., J. Med. Chem.; 1999; 42(19); 4001-4009.

4.8.63. Solid-Phase Strategies for the Assembly of Template-Based Protein Mimetics1 Peluso, S., Dumy, P., Nkubana, C., Yokokawa, Y., Mutter, M., J. Org. Chem. 1999; 64(19); 7114-7120.

4.8.64. Learning Nature's Strategies for Making Deoxy Sugars: Pathways, Mechanisms, and Combinatorial Applications  Hallis, T. M., Liu, H.-w. Accounts of Chemical Research 1999; 32(7); 579-588.

4.8.65. Solid Phase synthesis of structurally diverse pyrimido [4,5-d] pyrimidines for the potential use in combinatorial chemistry Srivasta, S. K.; Haq, W.; Chauhan, P. M. Bioorg. Med. Chem. Lett. 1999, 9, 965-966.

4.8.66. An approach to enantiomerically pure inverse gamma-turn mimetics for use in solid-phase synthesis Brickmann, K., Somfai, P., & Kihlberg, J. 1997, Tetrahedron Lett. (38); 3651-3654.

4.8.67. Moenomycin A: New Chemistry that Allows to Attach the Antibiotic to Reporter Groups, Solid Support, and Proteins Kempin, U.; Hennig, L.; Knoll, D.; Welzel, P.; Muller, D.; Markus, A.; van Heijenoort, J  1997, Tetrahedron  53 (52); 17669-17690.

4.8.68. Solid-Phase synthesis of combinatorial libraries Lebl, M. 1999, Curr. Opin. Drug. Disc. Develop. 2, (4) 385-395.

4.8.69. Solid-Phase Synthesis of Large Tetrahydroisoquinoline Arrays by Two Different Approaches Lebl, M.; Krchnak, V.; Ibrahim, G.; Pires, J.; Burger, C.; Ni, Y.; Chen, Y.; Podue, D.; Mudra, P.; Pokorny, V.; Poncar, P.; Zenisek, K. 1999, Synthesis 11, 1971-1978.

4.8.70. Solid phase syntheses of oligoureas Burgess, K.; Ibarzo, J.; Linthicum, D.S.; Russell, D.H.; Shin, H.; Shitangkoon, A.; Totani, R.; Zhang, A.J. 1997, J. Amer. Chem. Soc. 119, 1556-1564.

4.8.71. Nanomolar Inhibitors for 2 Distinct Biological Target Families from a Single Synthetic Sequence - A Next Step in Combinatorial Library Design? Burns, C. J.; Groneberg, R. D.; Salvino, J. M.; Mcgeehan, G.; Condon, S. M.; Morris, R.; Morrissette, M.; Mathew, R.; Darnbrough, S.; Neuenschwander, K.; Scotese, A.; Djuric, S. W.; Ullrich, J.; Labaudiniere, R. Angew. Chem. Int. Ed. 1998, 37(20) 2848-2850.

4.8.72. Synthesis and screening of small molecule libraries active in binding to DNA Shipps, G.W.; Pryor, K.E.; Xian, J.; Skyler, D.A.; Davidson, E.H.; Rebek, J. Proc. Natl. Acad. Sci. USA 1997, 94, 11833-11838.

4.8.73. Higher order iminodiacetic acid libraries for probing protein-protein Interactions Boger, D. L.; Goldberg, J.; Jiang, W.; Chai, W.; Ducray, P.; Lee, J. K.; Ozer, R. S.; Andersson, C.-M Bioorg. Med. Chem. 1998, 6(8), 1347 -1378.

4.8.74. Combinatorial discovery process yields antimicrobial peptoids Ng, S.; Goodson, B.; Ehrhardt, A.; Moos, W. H.; Siani, M.; Winter, J. Bioorg. Med. Chem. 1999, 7(9), 1781-1785.

4.8.75. Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D Carroll, C. D.; Johnson, T. O.; Tao, S.; Lauri, G.; Orlowski, M.; Gluzman, I. Y.; Goldberg, D. E.; Dolle, R. E. Bioorg. Med. Chem. Lett. 1998, 8, 3203-3206.

4.8.76. Automated parallel synthesis of a tetrahydroisoquinolin-based library: Potential prolyl endopeptidase inhibitors Vendeville, S.; Bourel, L.; Davioud-Charvet, E.; Grellier, P.; Deprez, B.; Sergheraert, C. Bioorg. Med. Chem. Lett. 1999, 9, 437-442.

4.8.77. Discovery of Novel Pyridinopolyamines with Potent Antimicrobial Activity - Deconvolution of Mixtures Synthesized by Solution-Phase Combinatorial Chemistry An, H.Y.; Haly, B.D.; Cook, P.D. J. Med. Chem. 1998, 41(5) 706-716.

4.8.78. N-(2-Benzoylphenyl)-L-Tyrosine Ppar-Gamma Agonists - 2 - Structure-Activity Relationship and Optimization of the Phenyl Alkyl Ether Moiety Collins, J. L.; Blanchard, S. G.; Boswell, G. E.; Charifson, P. S.; Cobb, J. E.; Henke, B. R.; Hullryde, E. A.; Kazmierski, W. M.; Lake, D. H.; Leesnitzer, L. M.; Lehmann, J.; Lenhard, J. M.; Orbandmiller, L. A.; Graynunez, Y.; Parks, D. J.; Plunkett, K. D., and Tong, W. Q. J. Med. Chem. 1998, 41(25) 5037-5054.

4.8.79. Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecar-boxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): Coapplication of structure-based design and rapid multiple analogue synthesis on solid support Brady, S.F.; Stauffer, K.J.; Lumma, W.C.; Smith, G.M.; Ramjit, H.G.; Lewis, S.D.; Lucas, B.J.; Gardell, S.J.; Lyle, E.A.; Appleby, S.D.; Cook, J.J.; Holahan, M.A.; Stranieri, M.T.; Lynch, J.J.Jr.; Lin, J.H.; Chen, I.W.; Vastag, K.; Naylor-Olsen, A.M.; Vacca, J.P. J. Med. Chem. 1998, 41, 401-406.

4.8.80. Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: Identification of novel inhibitors of matrix metalloproteinases Szardenings, A.K.; Harris, D.; Lam, S.; Shi, L.; Tien, D.; Wang, Y.; Patel, D.V.; Navre, M.; Campbell, D.A. J. Med. Chem. 1998, 41, 2194-2200.

4.8.81. Design of Novel, Potent, Noncovalent Inhibitors of Thrombin with Nonbasic P-1 Substructures: Rapid Structure-Activity Studies by Solid-Phase Synthesis Lumma, W. C.; Witherup, K. M.; Tucker, T. J.; Brady, S. F.; Sisko, J. T.; Naylorolsen, A. M.; Lewis, S. D.; Lucas, B. J., and Vacca, J. P. J. Med. Chem. 1998, 41(7) 1011-1013.

 


Chapter 5. Analytical Methods for Solid Phase Synthesis

5.1. Colormetric Assays on Solid Support


5.1.1. Rapid Fluorescence Determination of the Absolute Amount of Aldehyde and Ketone Groups on Resin Supports Yan, B.; Li, W. J. Org. Chem. 1997, 62, 9354-9357. 

5.2. Identification of Compounds Released from Resin

5.3. NMR Techniques for Solid-Phase Synthesis

5.3.1. Magic Angle Spinning NMR for Reaction Monitoring and Structure Determination of Molecules Attached to Multipin Crowns Chin, J.; Fell, B.; Shapiro, M. J.; Tomexch, J.; Wareing, J. R.; Bray, A. M. J. Org. Chem. 1997, 62, 538-539.

5.3.2. Enhanced Resolution in MAS NMR for Combinatorial Chemistry Shapiro, M. J.; Chin, J.; Marti, R. E.; Jarosinski, M. A. Tetrahedron Lett. 1997, 38, 1333-1336.

5.3.3. New Methods for Obtaining High-Resolution NMR Spectra of Solid-Phase Synthesis Resins, Natural Products, and Solution-State Combinatorial Chemistry Libraries Keifer, P. A. Drugs of the Future 1998, 23, 3, 301-317.

5.3.4. Probing the Scope of the Asymmetric Dihydroxylation of Polymer-Bound Olefins. Monitoring by HRMAS NMR Allows for Reaction Control and On-Bead Mesurement of Enantiomeric Excess Riedl, R.; Tappe, R.; Berkessel, A. J. Am. Chem. Soc. 1998, 120, 8994-9000.

5.3.5. Improved Procedure for Routine 13-C NMR Analysis of Merrifield Resin Bound Molecules Lorge, F.; Wagner, A.; Mioskowski, C. J. Combinatorial Chemistry 1999, 1, 1, 25-27.

5.3.6. Encoding of Combinatorial Chemistry Libraries by Fluorine-19 NMR Hochlowski, J. E.; Whittern, D. N.; Sowin, T. J. J. Combinatorial Chemistry 1999, 1, 4, 291-293.

5.3.7. Covalent or trapped? PFG diffusion MAS NMR for combinatorial chemistry M. J. Shapiro, J. Chin, A. Chen, J. R. Wareing, Q. Tang, R. A. Tommasi, H. R. Marepalli Tetrahedron Lett. 1999, 40(34), 6141-6144.

5.3.8. Screening mixtures by affinity NMR Lin, M.F., Shapiro, M.J., & Wareing, J.R. J. Org. Chem. 1997, 62, 8930-8931.

5.3.9. HPLC/NMR in combinatorial chemistry Chin, J., Fell, J.B., Jarosinski, M., Shapiro, M.J., & Wareing, J.R. 1998, J. Org. Chem. 63, 386-390.

5.3.10. 2D SECSY NMR for combinatorial chemistry: High-resolution MAS spectra for resin-bound molecules Chin, J., Fell, B., Pochapsky, S., Shapiro, M.J., & Wareing, J.R. 1998, J. Org. Chem. 63, 1309-1311.

5.3.11. Diffusion edited NMR: Screening compound mixtures by affinity NMR to detect binding ligands to vancomycin Bleicher, K., Lin, M.F., Shapiro, M.J., Wareing, J.R. 1998, J. Org. Chem. 63, 8486-8490.

5.3.12. Isocyanate-based dendritic building blocks: Combinatorial tier construction and macromolecular-property modification Newkome, G.R.; Weis, C.D.; Moorefield.C.N.; Baker, G.R.; Childs, B.J.; Epperson, J. Angew. Chem. Int. Ed. 1998, 37, 307-310. 

5.4. IR Techniques for Solid-Phase Synthesis

5.4.1. High Throughput On-Bead Monitoring of Solid Phase Reactions by Diffuse Reflectance Infrared Fourier Transform Spectroscopy (DRIFTS) Chan, T. Y.; Chen, R.; Sofia, M. J.; Smith, B. C.; Glennon, D. Tetrahedron Lett. 1997, 38, 2821-2824.

5.4.2. A Direct Comparison of the Mixing Efficiency in Solid-Phase Organic Synthesis by Single Bead IR and Fluorescence Spectroscopy Yan, B.; Li, W. Tetrahedron Lett. 1997, 38, 6485-6488.

5.4.3. Crucial Factors Regulating Site Interactions in Resin Supports Determined by Single Bead IR Yan, B.; Sun, Q. J. Org. Chem. 1997, 63, 55-58.

5.4.4. Characterization of Reaction Products on Solid Supports by FT-IR Deben, I. E. A.; van Wijk, T, H, M.; van Doornum, E. M.; Hermkens, P. H. H.; Kellenbach, E. R. Mikrochim. Acta [Suppl.] 1997, 14, 245-246.

5.4.5. Monitoring the Progress and the Yield of Solid-Phase Organic Reactions Directly on Resin Supports Yan, B. Acc. Chem. Res. 1998, 31, 621-630.

5.4.6. Infrared and Raman Spectra of a Single Resin Bead for Analysis of Solid-Phase Reactions and Use in Encoding Combinatorial Libraries Rahman, S. S.; Busby, D. J.; Lee, D. C. J. Org. Chem. 1998, 63, 6196-6199.

5.4.7. A Comparison of Various FTIR and FT Raman Methods:  Applications in the Reaction Optimization Stage of Combinatorial Chemistry Yan, B.; Gremlich, H.-U.; Mos, S.; Coppola, G. M.; Sun, Q.; Liu, L. J. Combinatorial Chemistry 1999, 1, 1, 46-54.

5.4.8. Direct Infrared Spectroscopic Analysis of Reagent Partitioning in Polystyrene Bead Supported Solid Phase Reaction Chemistry Pivonka, D. E.; Palmer, D. L. J. Combinatorial Chemistry 1999, 1, 4, 294-296.

5.4.9. ESI Fourier Transform Ion Cyclotron Resonance Mass Spectrometry (ESI-FT-ICR-MS): A Rapid High-Resolution Analytical Method for Combinatorial Compound Libraries Walk, T. B.; Trautwein, A. W.; Richter, H.; Jung, G. Angew. Chem. Int. Ed. 1999, 38(12), 1763-1765.

5.4.10. Infrared and Raman-Spectroscopy in Combinatorial Chemistry Gremlich, H. U. American Laboratory 1998; 30(24):33-39.

5.4.11. Investigation of Solid-Phase Peptide Synthesis by the Near-Infrared Multispectral Imaging Technique: A Detection Method for Combinatorial Chemistry Fischer, M., Tran, C. D., Analytical Chemistry; 1999; 71(13); 2255-2261.

5.4.12. Fourier Transform Combinatorial Chemistry Schwabacher, A. W., Shen, Y., Johnson, C. W., J. Am. Chem. Soc.; 1999;121(37); 8669-8670.

5.4.13. Determination of the Absolute Amount of Resin-Bound Hydroxyl or Carboxyl Groups for the Optimization of Solid-Phase Combinatorial and Parallel Organic Synthesis  Yan, B., Liu, L., Astor, C. A., Tang, Q.  Analytical Chemistry; 1999; 71(20); 4564-4571.

5.4.14. Microdrift - Rapid and Efficient IR Analysis of Solid-Phase Organic-Chemistry Reactions Deben, I.; Goorden, J.; Vandoornum, E.; Ovaa, H., and Kellenbach, E. Eur. J. Org.Chem.; 1998; (4):697-700.

5.4.15. A case study of employing spectroscopic tools for monitoring reactions in the developmental stage of a combinatorial chemistry library Luo, Y., Ouyang, X.H., Armstrong, R.W., Murphy, M.M. 1998, J. Org. Chem. 63, 8719-8722.

5.4.16. Effects of polymer supports on the kinetics of solid-phase organic reactions: A comparison of polystyrene- and Tentagel-based resins Li, W., Yan, B. J. Org. Chem. 1998, 63, 4092-4097.

5.5. Mass Spectrometry Techniques for Solid-Phase Synthesis

5.5.1. Evaluation of Mass Spectrometric Methods Applicable to the Direct Analysis of Non-Peptide Bead-Bound Combinatorial Libraries Brummel, C. L.; Bickerman, J. C.; Carr, S. A.; Hemling, M. E.; Roberts, G. D.; Johnson, W.; Weinstock, J.; Gaitanopoulos, D.; Benkovic, S. J.; Winograd, N. Anal. Chem. 1996, 68, 237-242.

5.5.2. Spectrometrically Monitored Selection Experiments-Quantitative Laser Desorption Mass Spectrometry of Small Chemical Libraries Berlin, K.; Jain, R. K.; Tetzlaff, C.; Steinbeck, D.; Richert, C. Chem. Biol. 1997,4, 63-77.

5.5.3. Direct Monitoring of Organic Reactions on Polymeric Supports Carrasco, M. R.; Fitzgerald, M. C.; Oda, Y.; Kent, S. B. H. Tetrahedron Lett. 1997, 38, 6331-6334. 5.5.4. Probing combinatorial library diversity by mass spectrometry Demirev, P.A., & Zubarev, R.A. Anal. Chem. 1997, 69, 2893-2900.

5.5.5. Analysis of 9-fluorenylmethoxycarbonyl (Fmoc) loading of solid-phase synthesis resins by gas chromatography Newcomb, W.S., Deegan, T.L., Miller, W., & Porco, J.A.Jr. Biotech. Bioeng. (Comb. Chem.) 1998, 61, 55-60.

5.5.6. Microscale Frontal Affinity-Chromatography with Mass-Spectrometric Detection - A New Method for the Screening of Compound Libraries Schriemer, D. C.; Bundle, D. R.; Li, L., Hindsgaul, O. Angew. Chem. Int. Ed. 1998, 37(24) 3383-3387.

5.5.7. FT-IR Mapping -- A New Tool for Spatially-Resolved Characterization of Polymer-Bound Combinatorial Compound Libraries with Ir Microscopy Haap, W. J.; Walk, T. B.; Jung, G. Angew. Chem. Int. Ed. 1998, 37(23) 3311-3314.

5.5.8. Pulsed ultrafiltration mass spectrometry: A new method for screening combinatorial libraries van Breemen, R.B.; Huang, C.R.; Nikolic, D.; Woodbury, C.P.; Zhao, Y.Z.; Venton, D.L. 1997, Anal. Chem. 69, 2159-2164.

5.5.9. Design of self-coded combinatorial libraries to facilitate direct analysis of ligands by mass spectrometry Hughes, I. J. Med. Chem. 1998, 41, 3804-3811. 

5.6. Other Analytical Methods for Combinatorial Synthesis

5.6.1. Chemiluminescent Nitrogen Detection for HPLC: An Important New Tool in Organic Analytical Chemistry Fitch, W. L.; Szardenings, A. K.; Fujinari, E. M. Tetrahedron Lett. 1997, 38, 1689-1692.

5.6.2. Monitoring Solid Phase Reactions with Ion-Selective Electrode Patek, M.; Bildstein, S.; Flegelova, Z. Tetrahedron Lett. 1998, 39, 753-756.

5.6.3. A New Method for the Characterization of Chemical Libraries--Solely by HPLC Retention Times von Roedern, E. G. Molecular Diversity 1998, 3, 253-256.

5.6.4. Preparation of Spin-Labeled Styrene-Divinylbenzene Copolymers and a New
Approach for Quantitative Determination of the Resin Loading Using ESR Spectroscopy
Katritzky, A. R.; Belyakov, S. A.; Strah, S.; Cage, B.; Dalal, N. S.
Tetrahedron Lett., 1999, 40, 3, 407-410.

5.6.5. High-Throughput Characterization of Combinatorial Libraries Generated by Parallel Synthesis Kyranos, J. N.;  Hogan, J. C. Anal. Chem. 1998; 70(11):A389-A395 (Review).

5.6.6. Fast Gradient RP-HPLC for High-Throughput Quality-Control Analysis of Spatially Addressable Combinatorial Libraries Goetzinger, W. K. and Kyranos, J. N. American Laboratory 1998; 30, (8), 27.

5.6.7. A photolabile carbamate based dual linker analytical construct for facile monitoring of solid phase chemistry: 'TLC' for solid phase? S. C. McKeown, S. P. Watson, R. A. E. Carr, P. Marshall Heyer, Tetrahedron Lett. 1999, 40(12), 2407-2410.

5.6.8.  Screening of Mixture Combinatorial Libraries for Chiral Selectors: A Reciprocal Chromatographic Approach Using Enantiomeric Libraries Wu, Y.,Wang, Y.,Yang, A.,Li, T., Anal. Chem. 1999, 71(9), 1688-1691.

5.6.9. Rapid reaction scanning of solid phase chemistry using resins incorporating analytical constructs P. J. Murray, C. Kay, J. J. Scicinski, S. C. McKeown, S. P. Watson, R. A. E. Carr Tetrahedron Lett. 1999,40(30), 5609-5612.

5.6.10. Automated Electrochemical Analysis with Combinatorial Electrode Arrays  Sullivan, M. G., Utomo, H., Fagan, P. J., Ward, M. D., Analytical Chemistry 1999, 71(19), 4369-4375.

5.6.11. Analytical methods for quality control of combinatorial libraries Fitch, W. L., Mol. Diversity 1999, (4), 39-45.

5.6.12. Immunoaffinity ultrafiltration with ion spray HPLC/MS for screening small-molecule libraries Wieboldt, R., Zweigenbaum, J., Henion, J. Anal. Chem. 1997, (69) 1683-1691.

5.6.13. A fluorescence-based assay for high-throughput screening of coupling reactions. Application to Heck chemistry Shaughnessy, K.H., Kim, P., & Hartwig, J.F. J. Amer. Chem. Soc. 1999, 121, 2123-2132.

5.6.14. Rapid reaction scanning of solid phase chemistry using resins incorporating analytical constructs Murray, P. J.; Kay, C.; Scicinski, J. J.; McKeown, S. C.; Watson, S. P.; Carr, R. A. E. Tetrahedron Lett. 1999, 40(30), 5609-5612.

 


Chapter 6. Solution Libraries and the Solution/Solid-Phase Interface

6.1. Solution Libraries

6.1.1. Fluorous Synthesis: A Fluorous-Phase Strategy for Improving Separation Efficiency in Organic Synthesis Studer, A.; Hadida, S.; Ferritto, R.; Kim, S.-Y.; Jeger, P.; Wipf, P.; Curran, D. P. Science 1997, 275, 823-826.

6.1.2. Fluorous Synthesis: Fluorous Protocols for the Ugi and Biginelli Multicomponent Condensations Studer, A.; Jeger, P.; Wipf, P.; Curran, D. P. J. Org. Chem. 1997, 62, 2917-2924.

6.1.3. Solution Phase Combinatorial Chemistry. Discovery of Noval Polyazapyridinophanes with Potent Antibacterial Activity by a Solution Phase Simultaneous Addition of Functionalities Approach An, H.; Cummins, L. L.; Griffey, R. H.; Bharadwaj, R.; Haly, B. D.; Fraser, A. S.; Wilson-Lingardo, L.; Risen, L. M.; Wyatt, J. R.; Cook, P. D. J. Am. Chem. Soc. 1997, 119,3696-3708.

6.1.4. Solution-Phase Synthesis of a Combinatorial Thiohydantoin Library Sim, M. M.; Ganesan, A. J. Org. Chem. 1997, 62, 3230-3235.

6.1.5. Solution Phase Combinatorial Synthesis of Arylpiperazines Neuville, L.; Zhu, J. Tetrahedron Lett. 1997, 38, 4091-4094.

6.1.6. Rapid In-Plate Generation of Benzimidazole Libraries and Amide Formation Using EEDQ Thomas, J. B.; Fall, M. J.; Cooper, J. B.; Burgess, J. P.; Carroll, F. I. Tetrahedron Lett. 1997, 38, 5099-5102.

6.1.7. Solution-Phase Combinatorial Synthesis via the Olefin Metathesis Reaction Boger, D. L.; Chai, W.; Ozer, R. S.; Andersson, C.-M. Bioorg. Med. Chem. Lett. 1997, 7, 463-468.

6.1.8. Structure Optimization of a Leukotriene D4 Antagonist by Combinatorial Chemistry in Solution Maehr, H.; Yang, R. Bioorg. Med. Chem. 1997, 5, 493-496.

6.1.9. A New Diketopiperazine tetra-Carboxylic Acid as Template for the Homogeneous Phase Synthesis of Chemical Libraries Falorni, M.; Giacomelli, G.; Nieddu, F.; Taddei, M. Tetrahedron Lett. 1997, 38, 4663-4666.

6.1.10. Convergent Parallel Synthesis Baldino, C. M.; Casebier, D. S.; Caserta, J.; Slobodkin, G.; Tu, C; Coffen, D. L. Synlett1997, 488-490.

6.1.11. Generation of Targeted C2-Symmetrical Compound Libraries by Solution-Phase Combinatorial Chemistry Bioorg. Med. Chem. Lett. 1997, 7, 1903-1908.

6.1.12. Solution-Phase Synthesis of a beta-Amino Alcohol Combinatorial Library Chng, B. L.; Ganesan, A. Bioorg. Med. Chem. Lett. 1997, 7, 1511-1514.

6.1.13. A Strategic Alternative to Solid Phase Synthesis: Preparation of a Small Isoxazoline Library by "Fluorous Synthesis" Studer, A.; Curran, D. P. Tetrahedron 1997, 53, 6681-6696.

6.1.14. Palladium-Catalyzed Stille Couplings with Fluorous Tin Reactants Hoshino, M.; Degenkolb, P.; Curran, D. P. J. Org. Chem. 1997, 62, 8341-8349.

6.1.15. Synthesis and Activity of 2,6,9-Trisubstituted Purines Schow, S. R.; Mackman, R. L.; Blum, C. L.; Brooks, E.; Horsma, A.; Joly, A.; Kerwar, S. S.; Lee, G.; Shiffman, D.; Nelson, M. G.; Wang, X.; Wick, M. M.; Zhang, X.; Lum, R. T. Tetrahedron Lett. 1997, 7, 2697-2702.

6.1.16. Solution-Phase Synthesis of 2,6,9-Trisubstituted Purines Fiorini, M. T.; Abell, C. Tetrahedron Lett. 1998, 39, 1827-1830.

6.1.17. Solution-Phase Parallel Synthesis of Benzoxazines Using a Polymer-Supported Carbodiimide Buckman, B. O.; Morrissey, M. M.; Mohan, R. Tetrahedron Lett. 1998, 39, 1487-1488.

6.1.18. The Solution Phase Synthesis of Diketopiperazine Libraries via the Ugi Reaction: Novel Application of Armstrong's Convertible Isonitrile Hulme, C.; Morrissette, M. M.; Volz, F. A.; Burns, C. J. Tetrahedron Lett. 1998, 39, 1113-1116.

6.1.19. Microwave Assisted Combinatorial Chemistry, Synthesis of Substituted Pyridines Cotterill, I. C.; Usyatinsky, A. Y.; Arnold, J. M.; Clark, D. S.; Dordick, J. S.; Michels, P. C.; Khmelnitsky, Y. L. Tetrahedron Lett. 1998, 39, 1117-1120.

6.1.20. Novel Quenchers for Solution Phase Parallel Synthesis Nikam, S. S.; Kornberg, B. E.; Ault-Justus, S. E.; Rafferty, M. F. Tetrahedron Lett. 1998, 39, 1121-1124.

6.1.21. Solution-Phase Synthesis of Novel Linear Oxyamine Combinatorial Libraries with Antibacterial Activity Kung, P-P.; Bharadwaj, R.; Fraser, A. S.; Cook, D. R.; Kawasaki, A. M.; Cook, P. D. J. Org. Chem. 1998, 63, 1846-1852.

6.1.22. Poly(ethylene glycol) Supported Liquid Phase Synthesis of Biaryls Blettner, C. G.; Konig, W. A.; Stenzel, W.; Schotten, T. Synlett1998, 295-297.

6.1.23. Combinatorial Synthesis of Oligosaccharide Library of 2,6-Dideoxysugars Izumi, M.; Ichikawa, Y. Tetrahedron Lett. 1998, 39, 2079-2082.

6.1.24. Solution Phase Synthesis of a Spiro[pyrrolidine-2,3'-oxindole] Library via a Three Component 1,3-Dipolar Cycloaddition Reaction Fokas, D.; Ryan, W. J.; Casebier, D. S.; Coffen, D. L. Tetrahedron Lett. 1998, 39, 2235-2238.

6.1.25. A Solution-Phase Combinatorial Parallel Synthesis of 3-beta-Amido-3-alpha-hydroxy-5-alpha-androstane-17-ones Maltais, R.; Poirier, D. Tetrahedron Lett. 1998, 39, 4151-4154.

6.1.26. "Reagent Explosion": An Efficient Method to Increase Library Size and Diversity Bienayme, H. Tetrahedron Lett. 1998, 39, 4255-4258.

6.1.27. Libraries of N-Alkylaminoheterocycles from Nucleophilic Aromatic Substitution with Purification by Solid Supported Liquid Extraction Johnson, C. R.; Zhang, B.; Fantauzzi, P.; Hocker, M.; Yager, K. M. Tetrahedron 1998, 54, 4097-4106.

6.1.28. The Use of High-Throughput Synthesis and Purification in the Preparation of a Directed Library of Adrenergic Agents Siegel, M. G.; Shuker, A. J.; Droste, C. A.; Hahn, P. J.; Jesudason, C. D.; McDonald, J. H.; Matthews, D. P.; Rito, C. J.; Thorpe, A. J. Molecular Diversity1998, 3, 113-116.

6.1.29. Preparation of a Fluorous Benzyl Protecting Group and Its Use in a Fluorous Synthesis Approach to a Disaccharide  Curran, D. P.; Ferritto, R.; Hua, Y. Tetrahedron Lett. 1998, 39, 4937-4940.

6.1.30. Applications of N-BOC-Diamines for the Solution Phase Synthesis of Ketopiperazine Libraries Utilizing a Ugi/De-BOC/Cyclization (UDC) Strategy Hulme, C.; Peng, J.; Louridas, B.; Menard, P.; Krolikowski, P.; Kumar, N. V. Tetrahedron Lett. 1998, 39, 8047-8050.

6.1.31. Libraries of N-Alkylaminoheterocycles from Nucleophilic Aromatic Substitution with Purification by Solid Supported Liquid Extraction Johnson, C. R.; Zhang, B.; Fantauzzi, P.; Hocker, M.; Yager, K. M. Tetrahedron 1998, 54, 4097-4106.

6.1.32. Solution and Solid Phase Combinatorial Synthesis of Peptidomimetic Library Containing Diversified alpha-Methylated Amino Acids Kim, S. W.; Shin, Y. S.; Ro, S. Bioorg. Med. Chem. Lett. 1998, 8, 1665-1668.

6.1.33. Enhanced Diastereoselectivity in the Asymmetric Ugi Reaction Using a New "Convertible" Isonitrile Linderman, R. J.; Binet, S.; Petrich, S. R. J. Org. Chem. 1999, 64, 336-337.

6.1.34. Unique Structures Generated by Ugi 3CC Reactions Using Bifunctional Starting Materials Containing Aldehyde and Carboxylic Acid Zhang, J.; Jacobson, A.; Rusche, J. R.; Herlihy, W. J. Org. Chem. 1999, 64, 1074-1076.

6.1.35. Parallel Synthesis of Aminomethylphosphine Ligands LaPointe, A. M. J. Combinatorial Chemistry 1999, 1, 1, 101-104.

6.1.36. A Combinatorial Approach to Recognition of Chirality:  Preparation of Highly Enantioselective Aryl-Dihydropyrimidine Selectors for Chiral HPLC Lewandowski, K.; Murer, P.; Svec, F.; Frechet, J. M. J. J. Combinatorial Chemistry 1999, 1, 1, 105-112.

6.1.37. Solution Phase Combinatorial Synthesis of Biaryl Libraries Employing Heterogeneous Conditions for Catalysis and Isolation with Size Exclusion Chromatography for Purification Boger, D.; Goldberg, J.; Andersson, C.-M. J. Org. Chem. 1999, 64, 7, 2422-2427.

6.1.38. Submonomer Solution Synthesis of Hydrazinoazapeptoids, a New Class of Pseudopeptides Cheguillaume, A.; Lehardy, F.; Bouget, K.; Baudy-Floc'h, M.; Le Grel, P. J. Org. Chem. 1999, 64, 2924-2927.

6.1.39. Generation of a Library of 4-Thiazolidinones Utilizing Polymer-Supported Quench (Psq) Reagent Methodology Aultjustus, S. E.; Hodges, J. C., and Wilson, M. W . Biotechnol. Bioeng. 1998, 61(1):17-22.

6.1.40. Are Porphyrin Mixtures Favorable Photodynamic Anticancer Drugs - A Model Study with Combinatorial Libraries of Tetraphenylporphyrins Berlin, K.; Jain, R. K., and Richert, C. Biotechnol. Bioeng. 1998, 61(2):107-118.

6.1.41. A Convenient Method for Library Construction - Parallel Synthesis of Beta-Amino Ester and Quinoline Derivatives in Liquid-Phase Using Ln(Otf)(3)-Catalyzed 3-Component Reactions Kobayashi, S.; Komiyama, S., and Ishitani, H. Biotechnol. Bioeng. 1998,61(1):23-31.

6.1.42. Solution-Phase Library Generation - Methods and Applications in Drug Discovery Gayo, L. M.  Biotechnol. Bioeng. 1998, 61(2):95-106 (review).

6.1.43. Solution-Phase Simultaneous Addition of Functionalities (Spsaf) and Chemical Transformation to Prepare N,N'-Disubstituted Piperazine Libraries Kung, P. P. and Cook, P. D. Biotechnol. Bioeng. 1998, 61(2):119-125.

6.1.44. Rapid Synthesis of Matrix Metalloproteinase Inhibitors via Ugi 4-Component Condensation Floyd, C. D.; Harnett, L. A.; Miller, A.; Patel, S.; Saroglou, L., and Whittaker, M.  Synlett 1998,6, 637-639.

6.1.45.  Libraries for Receptor-Assisted Combinatorial Synthesis (Racs) - The Olefin Metathesis Reaction Giger, T.; Wigger, M.; Audetat, S., and Benner, S. A. Synlett 1998, 6, 688-691.

6.1.46. Synthesis of Imidazo(1,2-A) Annulated Pyridines, Pyrazines and Pyrimidines by a Novel 3-Component Condensation Groebke, K.; Weber, L., and Mehlin, F. Synlett 1998, 6, 661-663.

6.1.47. Rare-Earth Triflate-Catalyzed Addition-Reactions of Acylhydrazones with Silyl Enolates - A Facile Synthesis of Pyrazolone Derivatives Oyamada, H. and Kobayashi, S. Synlett 1998, 3, 249-250.

6.1.48. Design, Synthesis, and Evaluation of a Dye Library: Glass-Forming and Solid-State Luminescent Merocyanines for Functional Materials Würthner, F. ; Sens, R. ; Etzbach, K.-H.; Seybold, G. Angew. Chem. Int. Ed. 1999, 38(11), 1649-1652.

6.1.49. Libraries via Metathesis of Internal Olefins Brandli, C. and Ward, T. R.  Helv. Chim. Acta. 1998; 81(9):1616-1621.

6.1.50. Multisubstituted Urea Derivatives of Hydrazines by a Flexible Approach with Potential Application in Combinatorial Chemistry Grehn, L.; Ragnarsson, U. Synthesis-Stuttgart 1998; 12, 1817-1821.

6.1.51.  Detection of Benzodiazepine Receptor Ligands in Small Libraries of Flavone Derivatives Synthesized by Solution-Phase Combinatorial Chemistry Marder, M.; Viola, H.; Bacigaluppo, J. A.; Colombo, M. I.; Wasowski, C.; Wolfman, C.; Medina, J. H.; Ruveda, E. A.; Paladini, A. C. Biochem. Biophys. Res. Commun. 1998; 249(2), 481-485.

6.1.52.  Split-split. A multiple synthesiser approach to efficient automated parallel synthesis P. Brooking, A. Doran, P. Grimsey, N. W. Hird, W. S. MacLachlan, M. Vimal Oyamada, Tetrahedron Lett. 1999,40(7), 1405-1408.

6.1.53. 2-Pyridylsilyl group as a multifunctional 'phase tag' for solution phase synthesis J. Yoshida, K. Itami, K. Mitsudo, S. Suga, Tetrahedron Lett. 1999, 40(17), 3403-3406. 6.1.54. Amidine protection for solution phase library synthesis C. Bailey, E. Baker, J. Hayler, P. Kane, Tetrahedron Lett. 1999, 40(26), 4847-4850.

6.1.55. High-Speed, Highly Fluorous Organic Reactions Olofsson, K.; Kim, S.-Y.; Larhed, M.; Curran, D. P.; Hallberg, A. J. Org. Chem. 1999, 64, 12, 4539-4541.

6.1.56. Phosphorus(III) ligands with fluorous ponytails P. Bhattacharyya, D. Gudmunsen, E. G. Hope, R. D. W. Kemmitt, D. R. Paige, A. M. Stuart J.Chem.Soc. Perkin 1. 1997, 3609-3612.

6.1.57. Improved procedure for the solution phase preparation of 1,4-benzodiazepine-2,5-dione libraries via Armstrong's convertible isonitrile and the Ugi reaction Hulme, C.; Peng, J.; Tang, S.-Y.; Burns, C.J.; Morize, I.; Labaudiniere, R.  J. Org. Chem. 1998, 63, 8021-8023.

6.1.58. A solution-phase combinatorial chemistry methodology for drug discovery An, H.; Cook, P.D. Recent Res. Dev. Org. Chem. 1998,2, 473-488.

6.1.59. Liquid-phase synthesis of 2-(alkylthio) benzimidazoles C.-M. Yeh, C.-M. Sun Tetrahedron Lett., 1999, 40, 7247-7250.

6.1.60. New methodology for high throughput solution-phase synthesis: affinity purification by using crown ether and ammonium ion interaction S. Zhang, K. Fukase, S. Kusumoto Tetrahedron Lett., 1999,40, 7479.

6.1.61. Convergent Solution-Phase Combinatorial Synthesis with Multiplication of Diversity through Rigid Biaryl and Diarylacetylene Couplings Boger, D. L., Jiang, W., Goldberg, J.  J. Org. Chem.; 1999; 64(19); 7094-7100.

6.1.62. Solution-phase parallel oxazole synthesis with TosMIC Kulkarni, B. A. ; Ganesan, A.  Tetrahedron Lett. 1999, 40(30), 5637-5638.

6.1.63. A Facile Solution and Solid Phase Synthesis of Phosphotyrosine Mimetic L-4-[DiethylPhosphono(difluoromethyl)]-Phenylalanine (F2Pmp(EtO)2) Derivatives Qabar, M. N.; Urban, J.; Kahn, M.  Tetrahedron  1999, 53(32), 11171-11178.

6.1.64. Solution and Soluble Polymer Syntheses of 3-Aminoimidazoline-2,4-Diones Yoon, J. Y.; Cho, C. W.; Han, H., and Janda, K. D. Chem. Comm. 1998; (24) 2703-2704.

6.1.65. Solution-Phase Combinatorial Synthesis of 4-Hydroxyquinolin-2(1H)-Ones. Kulkarni, B. A. and Ganesan, A. Chem. Comm. 1998; (7):785-786.

6.1.66. Solution phase combinatorial chemistry. Synthesis of novel linear pyridinopolyamine libraries with potent antibacterial activity An, H.Y., Haly, B.D., Fraser, A.S., Guinosso, C.J., & Cook, P.D. J. Org. Chem. 1997, 62, 5156-5164.

6.1.67. Multistep convergent solution-phase combinatorial synthesis and deletion synthesis deconvolution Boger, D.L., Chai, W., & Jin, Q. 1998, J. Amer. Chem. Soc. 120, 7220-7225.

6.1.68. Combinatorial mixture synthesis and biological evaluation of dihydrophenyl triazine antifolates Lee, H.-K.; Chui, W.-K. Bioorg. Med. Chem. 1999, 7(6), 1255-1262.

6.1.69. Solution-phase combinatorial synthesis of ureas using nitrophenylcarbamates Raju, B.; Kassir, J. M.; Kogan, T. P. Bioorg. Med. Chem. Lett. 1998, 8, 3043-3048.

6.1.70. Liquid phase parallel synthesis of iminodiacetic acid derivatives Cheng, S.; Comer, D. D.; Myers, P. L.; Saunders, J. Tetrahedron Lett. 1999, 40(51), 8975-8978.

6.1.71. Solution-phase parallel synthesis using ion-exchange resins Suto, M. J.; Gayo-Fung, L. M.; Palanki, M. S. S.; Sullivan, R. Tetrahedron 1998, 54(16), 4141-4150.
 

6.2. Resin Capture

6.2.1. Ion-Exchange Resins for Solution Phase Parallel Synthesis of Chemical Libraries Gayo, L. M.; Suto, M. J. Tetrahedron Lett. 1997, 38, 513-516.

6.2.2. Rapid Purification of Small Molecule Libraries by Ion Exchange Chromatography Siegel, M. G.; Hahn, P. J.; Dressman, B. A.; Fritz, J. E.; Grunwell, J. R.; Kaldor, S. W. Tetrahedron Lett. 1997, 38, 3357-3360.

6.2.3. Parallel Synthesis of Tamoxifen and Derivatives on Solid Support via Resin Capture Brown, S. D.; Armstrong, R. W. J. Org. Chem. 1997, 62, 7076-7707.

6.2.4. The Application of High-Throughput Synthesis and Purification to the Preparation of Ethanolamines Shuker, A. J.; Siegel, M. G.; Matthews, D. P.; Weigel, L. O. Tetrahedron Lett. 1997, 38, 6149-6152.

6.2.5. Simultaneous Deprotection and Purification of BOC-amines Based on Ionic Resin Capture Liu, Y-S.; Zao, C.; Bergreiter, D. E.; Romo, D. J. Org. Chem. 1998, 63, 3471-3473.

6.2.6. Polymer-Assisted Solution Phase (PASP) Chemical Library Synthesis Flynn, D. L.; Devraj, R. V.; Naing, W.; Parlow, J. J.; Weidner, J. J.; Yang, S. Med. Chem. Res. 1998,  8, 219-243.

6.2.7. Polymer-Assisted Solution Phase Synthesis: A General Method for Sequestration of By-Products Formed from Activated Acyl-Transfer Reactants Weidner, J. J.; Parlow, J. J.; Flynn, D. L. Tetrahedron Lett., 1999, 40, 2, 239-242.

6.2.8. Parallel synthesis of 2-alkoxy and 2-acyloxyphenylpropylamides and amines using dihydrocoumarins as versatile synthons. Application of a novel resin quench capture method J. C. Bussolari, D. C. Rehborn, D. W. Combs, Tetrahedron Lett. 1999, 40, 7, 1241-1244. 

6.3. Support-Bound Reagents

6.3.1. Versatile Acylation of N-Nucleophiles Using a New Polymer-Supported 1-Hydroxybenzotriazole Derivative Pop, I. E.; Deprez, B. P.; Tartar, A. L. J. Org. Chem. 1997, 62, 2594-2603.

6.3.2. Polymer-bound Palladium-catalyzed Cross-coupling of Organoboron Compounds with Organic Halides and Organic Triflates Jang, S-B. Tetrahedron Lett. 1997, 38, 1793-1796.

6.3.3. Versatile Acylation of N-Nucleophiles Using a New Polymer-Supported 1-Hydroxybenzotriazole Derivative Pop, I. E.; Deprez, B. P.; Tartar, A. L. J. Org. Chem. 1997, 119, 2594-2604.

6.3.4. New Amphiphilic Palladium-Phosphine Complexes Bound to Solid Supports: Preparation and Use for Catalytic Allylic Substitution in Aqueous Media Uozumi, Y.; Danjo, H.; Hayashi, T. Tetrahedron Lett. 1997, 38, 3557-3560.

6.3.5. In Defense of the Catalytic Asymmetric Cis Dihydroxylation of Olefins Utilizing Insoluble Polymeric Ligand Slavadori, P.; Pini, D.; Petri, A. J. Am. Chem. Soc. 1997, 119, 6929-6930.

6.3.6. Preparation, Characterization, and Synthetic Uses of Lanthanide(III) Catalysts Supported on Ion Exchange Resins Yu, L.; Chen, D.; Li, J.; Wang, P. G. J. Org. Chem. 1997, 62, 3575-3581.

6.3.7. Chemical Library Purification Strategies Based on Principles of Complementary Molecular Reactivity and Molecular Recognition Flynn, D. L.; Crich, J. Z.; Devraj, R. V.; Hockerman, S. L.; Parlow, J. J.; South, M. S.; Woodard, S. J. Am. Chem. Soc. 1997, 119, 4874-4881.

6.3.8. Polymer-Supported Quenching Reagents for Parallel Purification Booth, R. J.; Hodges, J. C. J. Am. Chem. Soc. 1997, 119, 4882-4886.

6.3.9. Discovery of Antirhinoviral Leads by Screening a Combinatorial Library of Ureas Prepared Using Covalent Scavengers Kaldor, S. W.; Fritz, J. E.; Tang, J.; McKinney, E. R. Bioorg. Med. Chem. Lett. 1996, 6, 3041-3044.

6.3.10. In Situ Chemical Tagging: Tetrafluorophthalic Anhydride as a "Sequestration Enabling Reagent" (SER) in the Purification of Solution-Phase Combinatorial Libraries Parlow, J. J.; Naing, W.; South, M. S.; Flynn, D. L. Tetrahedron Lett. 1997, 38, 7959-7962.

6.3.11. Polymer Supported Bases in Combinatorial Chemistry: Synthesis of Aryl Ethers from Phenols and Alkyl Halides and Aryl Halides Xu, W.; Mohan, R.; Morrissey, M. M. Tetrahedron Lett. 1997, 38, 7337-7340.

6.3.12. Thermal Allylations of Aldehydes with a Fluorous Allylstannane. Separation of Organic and Fluorous Products by Solid Phase Extraction with Fluorous Reverse Phase Silica Gel Curran, D. P.; Hadida, S.; He, M. J. Org. Chem. 1997, 62, 6714-6715.

6.3.13. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'-bis(trifluoromethyl)phenyl)-carboxamide: A Potent Inhibitor of NF-kappaB- and AP-1-Mediated Gene Expression Identified Using Solution-Phase Combinatorial Chemistry Sullivan, R. W.; Bigam, C. G.; Erdman, P. E.; Palanki, M. S. S.; Anderson, D. W.; Goldman, M. E.; Ransone, L. J.; Suto, M. J. J. Med. Chem. 1998, 41, 413-419.

6.3.14. A Soluble Polymer Approach to the "Fishing Out" Principle: Synthesis and Purification of beta-Amino Alcohols Hori, M.; Janda, K. D. J. Org. Chem. 1998, 63, 889-894.

6.3.15. Polyethylene Glycol (PEG) as Polymeric Support and Phase-transfer Catalyst in the Soluble Polymer Liquid Phase Synthesis of alpha-Amino Esters Sauvagnat, B.; Lamaty, F.; Lazaro, R.; Martinez, J. Tetrahedron Lett. 1998, 39, 821-824.

6.3.16. Applications of Free and Resin-bound Novel (Trifluoromethyl)dioxiranes Boehlow, T. R.; Buxton, P. C.; Grocock, E. L.; Marples, B. A.; Waddington, V. L. Tetrahedron Lett. 1998, 39, 1839-1842.

6.3.17. Synthesis of N-Hydroxysuccinimide Esters Using Polymer Bound HOBt Dendrinos, K. G.; Kalivretenos, A. G. Tetrahedron Lett. 1998, 39, 1321-1324.

6.3.18. Modification of the Swern Oxidation: Use of a Soluble Polymer-Bound, Recyclable, and Odorless Sulfoxide Harris, J. M.; Liu, Y.; Chai, S.; Andrews, M. D.; Vederas, J. C. J. Org. Chem. 1998, 63, 2407-2409.

6.3.19. A Microencapsulated Lewis Acid. A New Type of Polymer-Supported Lewis Acid Catalyst of Wide Utility in Organic Synthesis Kobayashi, S.; Nagayama, S. J. Am. Chem. Soc. 1998, 120, 2985-2986.

6.3.20. Investigation of a New Family of Chiral Ligands for Enantioselective Catalysis via Parallel Synthesis and High-Throughput Screening Gennari, C.; Ceccarelli, S.; Piarulli, U.; Montalbetti, C. A. G. N.; Jackson, R. F. W. J. Org. Chem. 1998, 63, 5312-5313.

6.3.21. Unprecedented Polymer-Supported pi-Acid: Synthesis and Its Application as a Promoter to the Monthioacetalization of Acetals Masaki, Y.; Tanaka, N.; Miura, T. Tetrahedron Lett. 1998, 39, 5799-5802.

6.3.22. A Convenient Method for the Preparation of Acylsulfonamide Libraries Sturino, C. F.; Labelle, M. Tetrahedron Lett. 1998, 39, 5891-5894.

6.3.23. Palladium-Catalyzed Asymmetric Allylic Substitution in Aqueous Media Using Amphiphilic Resin-Supported MOP Ligands Uozumi, Y.; Danjo, H.; Hayashi, T. Tetrahedron Lett. 1998, 39, 8303-8306.

6.3.24. A New Scavenger Resin for Amines Coppola, G. M. Tetrahedron Lett. 1998, 39, 8233-8236.

6.3.25. Synthesis of Dipeptides Using Polymer Bound Hydroxamic Esters--A Comparative Study of Reactivity Sophiamma, P. N.; Sreekumar, K. Indian Journal of Chemistry 1997, 36B, 995-999.

6.3.26. High Catalytic Activity of Chiral Amino Alcohol Ligands Anchored to Polystyrene Resins Vidal-Ferran, A.; Bampos, N.; Moyano, A.; Pericas, M. A.; Riera, A.; Sanders, J. K. M. J. Org. Chem. 1998, 63, 6309-6318.

6.3.27. Polyaniline-Supported Cobalt Catalyst: A Three-Component Condensation Route to beta-Amino Acid Derivatives Prabhakaran, E. N.; Iqbal, J. J. Org. Chem. 1999, 64, 3339-3341.

6.3.28. Cross-Coupling of Aryl Halides and Allyl Acetates with Arylboron Reagents in Water Using an Amphiphilic Resin-Supported Palladium Catalyst Uozumi, Y.; Danjo, H.; Hayashi, T. J. Org. Chem. 1999, 64, 3384-3388.

6.3.29. Solid Phase Synthesis of Anhydrides and Amides - Polymer-Assisted Reaction in the Synthesis of Dipeptides  Rodriguez, J. G.; Martinvillamil, R., Ramos, S. New J. Chem. 1998; 22(8), 865-868.

6.3.30. High-Throughput Synthesis of Boc-Substituted Amidinoureas by Liquid-Phase Approach Sun, C.-M.; Shey, J.-Y. J. Combinatorial Chemistry 1999, 1, 5, 361-363.

6.3.31. Multipolymer-Supported Substrate and Ligand Approach to the Sharpless Asymmetric Dihydroxylation H. Han, K. D. Janda Angew.Chem.Int.Ed.1997,36, 1731-1733.

6.3.32. Polymer-supported solution synthesis of heparan sulphate-like oligomers Dreef-Tromp, C.M., Willems, H.A.M., Westerduin, P., van Veelen, P., & van Boeckel, C.A.A. Bioorg. Med. Chem. Lett., 1997,7, 1175-1180.

.3.33.  Clean three-step synthesis of 4,5-dihydro-1H-pyrazoles starting from alcohols using polymer supported reagents Haunert, F.; Bolli, M.H.; Hinzen, B.; Ley, S.V. J. Chem. Soc. Perkin Trans. 11998, 2235-2237.

6.3.34. Use of polymer supported reagents for clean multistep organic synthesis: preparation of amines and amine derivatives from  alcohols for use in compound library generation Ley, S.V.; Bolli, M.H.; Hinzen, B.; Gervois, A.-G.; Hall, B.J.  J.Chem. Soc. Perkin Trans. 1, 1998, 2239-2241.

6.3.35. A high throughput synthesis of aryl triflate and aryl nonaflate promoted by a polymer supported base (PTBD) S. Boisnard, J. Chastanet, J. Zhu Tetrahedron Lett., 1999, 40, 7469.

6.3.36. Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents M. Caldarelli, J. Habermann, S. V. Ley Bioorg. Med. Chem. Lett. 1999, 9(14), 2049.

6.3.37. An easily prepared, air and moisture stable, resin-bound palladium catalyst for Suzuki cross-coupling reactions T. Y. Zhang, M. J. Allen Tetrahedron Lett. 1999, 40(32), 5813-5816.

6.3.38. New solid phase Knoevenagel catalyst J. Simpson, D. L. Rathbone, D. C. Billington Tetrahedron Lett. 1999, 40(38), 7031-7034.

6.3.39. Purification of combinatorial libraries H. N. WellerMol. Diversity 1999, (4), 47-52.

6.3.40. Polyaniline supported cobalt(II)-salen catalyst: One pot synthesis of beta-phenylisoserine derivatives from cinnamoyl amide Das, B.C., Iqbal, J. Tetrahedron Lett. 1997, (38), 2903-2906.

6.3.41. Amphoteric, Water-Soluble Polymer-Bound Hydrogenation Catalysts Bergbreiter, D. E.; Liu, Y.-S.Tetrahedron Lett. 1997, (38), 3703-3706.

6.3.42. Water-Soluble Polymer-Bound, Recoverable Palladium(0)-Phosphine Catalysts Bergbreiter, D. E.; Liu, Y.-S.Tetrahedron Lett. 1997, (38), 7843-7846.

6.3.43 . Polymer-Supported Selenium Reagents for Organic-Synthesis Nicolaou, K. C.; Pastor, J.; Barluenga, S., and Winssinger, N. Chem. Comm. 1998, (18), 1947-1948.

6.3.44. Polymer supported alkali metal naphthalenides: Application in the generation of lithium and sodium reagents Van den Ancker, T.R., Hanson, G.R., Lee, F.C., & Raston, C.L. J. Chem. Soc. Chem. Commun. 1997, 125-126.

6.3.45. Polyaniline supported cobalt (II) salen catalyzed synthesis of pyrrolidine containing alpha-hydroxyamide core structures as inhibitors for HIV proteases Punniyamurthy, T., Iqbal, J. Tetrahedron Lett. 1997, 38, 4463-4466.

6.3.46. Palladium catalyzed Heck reactions and allylic substitution reactions using glass bead technology Tonks, L., Anson, M.S., Hellgardt, K., Mirza, A.R., Thompson, D.F., & Williams, J.M.J. Tetrahedron Lett. 1997, 38, 4319-4322.

6.3.47. Polymer-grafted Ti-TADDOL complexes. Preparation and use as catalysts in Diel-Alder reactions. Altava, B., Burguete, M.I., Escuder, B., Luis, S.V., & Salvador, R.V. J. Org. Chem. 1997, 62, 3126-3134.

6.3.48. A new, efficient, and in some cases highly regioselective water-soluble polymer rhodium catalyst for olefin hydroformylation Ajjou, A.N., Alper, H. J. Amer. Chem. Soc. 1998, 120, 1466-1468.

6.3.49. Schiff base catalysts for the asymmetric Strecker reaction identified and optimized from parallel synthetic libraries Sigman, M.S., & Jacobsen, E.N. J. Amer. Chem. Soc. 1998, 120, 4901-4902.

6.3.50. Functionalized cross-linked copolymers: A "C2-symmetric" solid-phase catalyst for enantioselective reactions Halm, C., & Kurth, M.J. Angew. Chem. Int. Ed. 1998, 37, 510-512.

6.3.51. Direct conversion of benzyl alcohol to ketone by polymer-supported Rh catalyst Jun, C-.H.; Hong, H.-S.; Huh, C.-W. Tetrahedron Lett. 1999, 40(50), 8897-8900.

6.3.52. Polymer supported naphthalene-catalysed lithiation reactions Gomez, C.; Ruiz, S.; Yus, M. Tetrahedron Lett. 1998, 39, 1397-1400.

6.3.53. Synthesis of polymer-bound Fischer chromium alkoxy and aminocarbene complexes Maiorana, S.; Seneci, P.; Rossi, T.; Baldoli, C.; Ciraco, M.; de Magistris, E.; Licandro, E.; Papagni, A.; Provera, S. Tetrahedron Lett. 1999, 40, 3635-3638.