Analytical Methods in Combinatorial Chemistry: (Critical Reviews in Combinatorial Chemistry)

This volume summarizes most analytical technologies that are applied to solving various problems in broad areas of combinatorial chemistry: chemistry optimization, library synthesis, lead selection, and lead optimization. It also suggests many avenues for further research, especially the need for major breakthroughs to resolve the incompatibility between parallel synthesis and the serial analysis and purification.Filling the tremendous need for analytical methodologies in various phases of combinatorial chemistry, this book will be a necessary addition to the library of anyone using combinatorial chemistry. While there are several resources available on the subject, there are no other books that deal specifically with analytical issues in combinatorial chemistry. Not only an ideal companion to the comprehensive reference books used by chemists in combinatorial chemistry, it is a timely textbook for university and graduate students, introducing them to the updated applications of modern analytical technologies in the rapidly growing field of combinatorial chemistry.F rom the Preface:This book is organized according to the operation process of combinatorial chemistry starting with the description of the basic properties of solid supports and their effects on solid-phase organic reactions in Chapter 2. Chapters 3-5 describe analytical methods routinely applied to the tedious process of reaction optimization. These techniques are various FTIR and Raman methods, MS, NMR, UV-Vis, fluorescence, and other analytical methods...Then the discussions move to the analytical control of the library quality in Chapter 6. The various methods for selecting active lead components from combinatorial libraries and the ways to reveal their structure or identity are discussed next in Chapter 7...The applications of analytical methods in the optimization of the in vitro activity and physicochemical properties of lead compounds are then illustrated in Chapter 8...Some promising new technologies and future perspectives are presented in Chapter 9.

Table of Contents:
Preface Acknowledgments Analytical Issues in Combinatorial Chemistry Combinatorial Chemistry Synthesis Methods Analytical Challenges An Examination of the Resin Support Physical Properties of Resins Effects of Swelling of Resin The Effects of Support Solvation on SPPS Summary Solid-Phase Reaction Optimization Using FTIR Methods Comparison of FTIR and Raman Techniques The Monitoring of Reactions on Polystyrene-Based Resin The Monitoring of Reactions on PS-PEG Resins: Comparing the Reaction Rate on PS and PS-PEG Resins The Monitoring of Reactions on Multipin Crowns Summary Reaction Optimization Using MS and NMR Methods MS Methods NMR Methods Summary Reaction Optimization Using Spectrophotometric, Fluorometric and Other Methods Qualitative Analysis of Amines Quantitative Analysis of Amines Quantitative Spectroscopic Methods for OrganicFunctional Groups Combustion Elemental Analysis Methods Electrochemical Methods On-Resin X-Ray, EPR, and Fluorescence Methods Summary Quality Control of Combinatorial Libraries Analysis of Discrete Compound Libraries Analysis of Pooled Libraries HPLC For Analyzing Compounds from Discrete and Mixture Libraries Summary Selection of Active Compounds from Combinatorial Libraries In-Solution Screening of Combinatorial Libraries Affinity Selection of Lead Compounds by Mass Spectrometry Affinity Capillary Electrophoresis Affinity NMR Other Affinity Selection Methods Encoding Methods Summary Optimization of Lead Compounds Lead Compounds and Lead Optimization Optimizing the in vitro Activity: SAR by NMR Optimizing Physicochemical Properties Summary Final Thoughts and Future Perspectives

Review :
"This book is the first comprehensive treatise covering all aspects of the complex problem of analysis of combinatorial chemistry libraries... The book is an essential addition to the library of anyone wishing to obtain a good overall review of the field of combinatorial chemistry and of its evolution and future development." -Journal of Medicinal Chemistry, 2001, vol. 44, no. 20