Quality measurement, control, and improvement in combinatorial
chemistry
Combinatorial chemistry has developed rapidly in the past decade,
with great advances made by scientists working on analysis and
purification of a large number of compounds and the analysis of
polymer-bound compounds. However, formidable challenges lie ahead
of today’s researcher. For example, high-throughput analysis and
purification technologies must be further developed to ensure
combinatorial libraries are 'purifiable, ’ and 'drugable.’
To this end, Analysis and Purification Methods in Combinatorial
Chemistry describes various analytical techniques and systems for
the development, validation, quality control, purification, and
physicochemical testing of combinatorial libraries. A new volume in
Wiley’s Chemical Analysis series, this text has four parts
covering:
* Various approaches to monitoring reactions on solid support and
optimizing reactions for library synthesis
* High-throughput analytical methods used to analyze the quality of
libraries
* High-throughput purification techniques
* Analytical methods applied in post-synthesis and
post-purification stages
Drawing from the contributions of respected experts in
combinatorial chemistry, this comprehensive book provides coverage
of applications of Nuclear Magnetic Resonance (NMR), liquid
chromatography/mass spectrometry (LC/MS), Fourier Transform
Infrared (FTIR), micellar electrokinetic chromatography (MEKC)
technologies, as well as other analytical techniques.
This eminently useful volume is an essential addition to the
library of students and researchers studying or working in
analytical chemistry, combinatorial chemistry, medicinal chemistry,
organic chemistry, biotechnology, biochemistry, or biophysics.
Spis treści
Preface.
Contributors.
PART I: ANALYSIS FOR FEASIBILITY AND OPTIMIZATION OF LIBRARY
SYNTHESIS.
Chapter 1. Quantitative Analysis in Organic Synthesis with NMR
(L. Lucas & C. Larive).
Chapter 2. ¯19F Gel-phase NMR Spectroscopy for
Reaction Monitoring and Quantification of Resin Loading (J.
Salvino).
Chapter 3. The Application of Single-Bead FTIR and Color Test
for Reaction Monitoring and Building Block Validation in
Combinatorial Library Sysnthesis(J. Cournoyer, et al.).
Chapter 4. HR-MAS NMR Analysis of Compounds Attached to Polymer
Supports (M. Guinó & Y. de Miguel).
Chapter 5. Multivariate Tools for Real-Time Monitoring and
Optimization of Combinatorial Materials and Process
Conditions (R. Potyrailo, et al.).
Chapter 6. Mass Spectrometry and Soluble Polymeric Supports (C.
Enjalbal, et al.).
PART II: HIGH-THROUGHPUT ANALYSIS FOR LIBRARY QUALITY
CONTROL.
Chapter 7. High-Throughput NMR Techniques for Combinatorial
Chemical Library Analysis (T. Hou & D. Raftery).
Chapter 8. Micellar Electrokinetic Chromatography as a Tool for
Combinatorial Chemistry Analysis: Theory and Applications (P.
Simms).
Chapter 9. Characterization of Split-Pool Encoded Combinatorial
Libraries (J. Zhang & W. Fitch).
PART III: HIGH-THROUGHPUT PURIFICATION TO IMPROVE LIBRARY
QUALITY.
Cha pter 10. Strategies and Methods for Purifying Organic
Compounds and Combinatorial Libraries (J. Zhao, et al.).
Chapter 11. HTP of Combinatorial Chemistry Libraries (J.
Hochlowski).
Chapter 12. Practical HPLC in High Throughput Analysis and
Purification (H. Gumm & R. God).
PART IV: ANALYSIS FOR COMPOUND STABILITY AND DRUGABILITY.
Chapter 13. Organic Compound Stability in Large, Diverse
Phatmaceutical Screening Collection (K. Morand & X. Cheng).
Chapter 14. Quartz Crystal Microbalance in Biomolecular
Recognition (M. Tseng, et al.).
Chapter 15. High-Throughput Physicochemical Profiling: Potential
and Limitations (B. Faller).
Chapter 16. Solubility in the Design of Combinatorial Libraries
(C. Lipinski).
Chapter 17. High-Throughput Determination of Log D Values
by LC/MS Method (J. Villena, et al.).
Index.
O autorze
BING YAN, Ph D, was born in China and received his Ph D in
chemistry at Columbia University in 1990. He then worked at Cambridge
University and the University of Texas-Houston Medical School as a postdoctoral
fellow. From 1993 to 1999, he worked for Novartis in the Core Technologies area
of preclinical research in New Jersey. He is currently at the Discovery
Chemistry division of Discovery Partners International, Inc., in San Francisco.
His major research interests are drug discovery, optimization of solid-phase
and solution-phase combinatorial synthesis, high-throughput quantitative and
qualitative analysis, and high-throughput purification of combinatorial
libraries. He has written four books and published over seventy reviews and
research articles.
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