Analytical Methods in Combinatorial Chemistry

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ISBN 9781566768092
Cat# TX68098
 

Features

  • Provides the only text of its kind organized according to the actual process used in combinatorial chemistry
  • Identifies the main advantages and weaknesses of current technologies
  • Points to the many research possibilities in analytical methods development in combinatorial chemistry
  • Essential guide for chemists working at pharmaceutical companies, biotech companies, consumer and personal product companies as well as chemistry graduate students
  • Summary

    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.

    From 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

    Editorial Reviews

    "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