Solid-Supported Combinatorial and Parallel Synthesis of Small-Molecular-Weight Compound Libraries

Chapter and selected section headings: Introduction, Basic Concepts and Strategies. Opening remarks (D. Obrecht). Historical landmarks in solid-supported organic synthesis (D. Obrecht). Applications of solid-supported organic chemistry (D. Obrecht). The role of solid-supported chemistry in modern drug discovery (D. Obrecht). Solid supports (P. Ermert). Solid-supported reagents (P. Ermert). Synthetic strategies in combinatorial and parallel synthesis (D. Obrecht, T. Masquelin). Classification of reactive building blocks (D. Obrecht). Tagging and deconvolution (K. Sekanina). Diversity (planning/assessment) (P. Jeger). Analytical methods (P. Jeger). Robotic systems and workstations (D. Obrecht). Linear Assembly Strategies. Introduction. Peptides. Peptoids. Oligonucleotides. Oligosaccharides. Oligocarbamates and oligoureas. Peptide-nucleic acids (PNA). Library Synthesis in Solution Using Liquid-Liquid and Liquid-Solid Extractions and Polymer-Bound Reagents (C. Zumbrunn et al.). Applications of solution-phase multicomponent and multigeneration reactions. Applications of liquid-liquid phase extractions. Applications of liquid-solid phase extractions and polymer-bound scavengers. Applications of polymer-bound reagents. Applications of polymer-bound catalysts. Solution chemistry using temporary trapping of intermediates on solid support ("intermediate catch" or "resin capture"). Organic synthesis on soluble polymeric supports. Convergent Assembly Strategies on Solid Supports (J.M. Villalgordo). Multigeneration assembly strategies with single functional group liberation. Multigeneration assembly strategies using traceless linkers. Multicomponent assembly strategies with single functional group liberation. Multicomponent assembly strategy with cyclisation-assisted cleavage. Multigeneration assembly strategies with multidirectional cleavage. References. Subject Index.