edited by Bing Yan
and Anthony W. Czarnik

Reveals the premier methods for carrying out solid-phase synthesis validation and quality control!

Optimization of Solid-Phase Combinatorial Synthesis addresses the key topic in combinatorial synthesis—how to optimize the quality of a combinatorial library—by determining the usefulness of synthesized compounds, the reliability of biological assay results, and analyzing academic and industrial applications, real-world examples, and case studies of successful and unsuccessful technologies.

Introduces a four-step approach to full-blown optimization! Presenting guidelines for the translation of solution chemistry to solid-phase chemistry, Optimization of Solid-Phase Combinatorial Synthesis:

• outlines resin selection criteria, supports, and characterization methods
• reviews quantitation of standards for calibration, kinetic measurements of compound cleavage from resin, and bead encoding
• documents the use of single bead infrared spectroscopy as a versatile reaction monitoring tool for synthesis optimization
• covers methods used for conducting feasibility, validation, and rehearsal of library synthesis
• quantifies bulk-released compounds and estimates average concentration and synthesis yield
• considers application of the Hammett relationship to predict solid-state reactivity
• assesses the state of the art in multispectral imaging of resin-supported libraries

With contributions from nearly 30 experts in library synthesis strategy, purification, and characterization, Optimization of Solid-Phase Combinatorial Synthesis is an essential reference for organic, analytical, medicinal, pharmaceutical, computational, protein, and peptide chemists and biochemists; pharmacists; pharmacologists; molecular biologists; molecular and vibrational spectroscopists; and upper-level undergraduate and graduate students in these disciplines.

Contents

1. A System for the Development and Production of Small-Molecule Libraries
2. Quality Control of Combinatorial Libraries Encoded with Electrophoric Tags: A Case Study
3. How to Optimize Reactions for Solid-Phase Synthesis of Combinatorial Libraries Using RF-Tagged Microreactors
4. Key Factors in the Translation of Solution-Phase Chemistry to the Solid Phase
5. The Choice of Solid Support
6. Applications of Fluorine-19 NMR Spectroscopy to Combinatorial Chemistry
7. Optimization of Solid-Phase Organic Syntheses by Monitoring Reactions on Single Resin Beads Using FTIR Microspectroscopy Bing Yan,
8. Spectroscopic Techniques for Optimizing Combinatorial Reactions on Solid Supports
9. Analytical Methods in Library Feasibility and Rehearsal Studies
10. Approaches to Reaction Monitoring by Product Derivatization
11. Methods for Quantitative Analysis of Compound Cleavage from Solid-Phase Resins
12. Hammett Relationships and Solid-Phase Synthesis: The Application of a Classical Solution to a Modern Problem
13. Multispectral Imaging for the High Throughput Evaluation of Solid-Phase-Supported Chemical Libraries
14. Microwave Applications to the Optimization of Combinatorial Synthesis
15. Optimizing Solution-Phase Synthesis Using Solid-Phase Techniques

Index

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