Elsevier S & T

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

Obrecht, D.; Villalgordo, J.M.

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Table of contents
  • List of Contributorsvii
  • Table of Contentsix
  • Forewordxv
  • List of Abbreviationsxvii
  • Chapter 1. Introduction, Basic Concepts and Strategies1
  • 1.1. Opening remarks (DO)1
  • 1.2. Historical landmarks in solid-supported organic synthesis (DO)5
  • 1.3. Applications of solid-supported organic chemistry (DO)10
  • 1.4. The role of solid-supported chemistry in modern drug discovery (DO)17
  • 1.5. Solid supports (PE)24
  • 1.6. Solid-supported reagents (PE)44
  • 1.7. Linker molecules and cleavage strategies (BD, DO)85
  • 1.8. Synthetic strategies in combinatorial and parallel synthesis (DO, TM)105
  • 1.9. Classification of reactive building blocks (DO)127
  • 1.10. Tagging and deconvolution (KS)145
  • 1.11. Diversity (planning/assessment) (PJ)156
  • 1.12. Analytical methods (PJ)158
  • 1.13. Robotic systems and workstations (DO)160
  • References164
  • Chapter 2. Linear Assembly Strategies185
  • 2.1. Introduction185
  • 2.2. Peptides186
  • 2.3. Conformationally constrained peptides188
  • 2.4. Peptoids197
  • 2.5. Oligonucleotides200
  • 2.6. Oligosaccharides201
  • 2.7. Oiigocarbamates and oligoureas205
  • 2.8. Peptide-Nucleic acids (PNA)207
  • References208
  • Chapter 3. Library Synthesis in Solution Using Liquid-Liquid and Liquid-Solid Extractions and Polyme213
  • 3.1. General213
  • 3.2. Applications of solution-phase multicomponent and multigeneration reactions217
  • 3.3. Applications of liquid-liquid phase extractions222
  • 3.4. Applications of liquid-solid phase extractions and polymer-bound scavengers224
  • 3.5. Applications of polymer-bound reagents228
  • 3.6. Applications of polymer-bound catalysts235
  • 3.7. Solution chemistry using temporary trapping of intermediates on solid support ("intermediate ca246
  • 3.8. Organic synthesis on soluble polymeric supports252
  • References256
  • Chapter 4. Convergent Assembly Strategies on Solid Supports (JMV)259
  • 4.1. Multigeneration assembly strategies with single functional group liberation259
  • 4.2. Multigeneration assembly strategies using traceless linkers292
  • 4.3. Multicomponent assembly strategies with single functional group liberation300
  • 4.4. Multigeneration assembly strategies with cyclisation-assisted cleavage306
  • 4.5. Muiticomponent assembly strategy with cyclisation-assisted cleavage318
  • 4.6. Multigeneration assembly strategies with multidirectional cleavage319
  • References328
  • Outlook and future directions334
  • Subject Index335
  • Acknowledgements339
Book details
  • Vendor Elsevier S & T
  • SKU 9780080432588
  • ISBN-13 9780080517360
  • Author Obrecht, D.; Villalgordo, J.M.
  • Category Medical
  • Subject Pharmacy

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The words "Combinatorial Chemistry" have different meanings to different people, ranging from split and mix strategies to parallel synthesis using robots, and embracing the whole range of preparative chemistry from organic molecules, to catalyst ligands, and even inorganic solids. All of these activities have in common an attempt to expand the diversity of structure available to the chemist as well as the access to this diversity, permitting the discovery of new and valuable biological acid material properties. In this outstanding survey of combinatorial organic chemistry, the authors, Obrecht who has established a new combinatorial chemistry company called Polyphor, and Villalgardo have brought together the literature, including that from 1998, and have concisely analysed the applications and achievements of this new field. This work will be of value to all chemists engaged in preparative work, both in industry and academe.