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.

Since the publication of the benchmark first edition of this book, chemical library and combinatorial chemistry methods have developed into mature technologies. There have also been significant shifts in emphasis in combinatorial synthesis. Reflecting the growth in the field and the heightened focus on select areas, Analytical Methods in Combinator

High Throughput Analysis for Early Drug Discovery offers concise and unbiased presentations by synthetic and analytical chemists who have been involved in creating and moving the field of combinatorial chemistry into the academic and industrial mainstream. Since the synthetic method often dictates the appropriate types of analysis, each chapter or section begins with a description of the synthesis approach and its advantages. The description of various combinatorial and high-throughput parallel synthesis techniques provide a relevant point of entry for synthetic chemists who need to set up appropriate characterisation methods for his/her organisation. This is an invaluable resource for all organic and analytical chemists in the pharmaceutical, agrochemical, and biotechnology fields who are either involved in, or beginning to investigate combinatorial techniques to increase overall efficiency and productivity. First reference to focus on the analytical side of synthesis

The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.

This volume aims to provide the necessary tools for developing methods and analyzing results in the drug discovery process, and supports documenting and managing the process in a combinatorial setting. It describes the chromatographic and spectroscopic techniques used to generate chemical and molecular diversity in new compounds, focusing on applications of information management systems, instrumentation, and robotics.

There is a vast and often bewildering array of synthetic methods and reagents available to organic chemists today. The Best Synthetic Methods series allows any scientist who is interested in the chemical transformations of molecules to choose between all the alternatives and assess their real advantages and limitations. With the emphasis on laboratory use, these volumes represent a comprehensive and practical guide to modern synthetic organic chemistry. This book is the product of the authors many years practical experience and reading of the original literature. It contains a valuable distillation and critical evaluation of the Best Synthetic Methods for the formation and reaction of thiophenes (five membered heterocycles containing a ring sulfur) or polymers containing a thiophene functionality (thienyls). A brief review of each area is provided, but the emphasis in all cases is on describing efficient practical methods to effect the transformations described. The reader can therefore use this book to rapidly review and select the best methods of performing a synthetic conversion to create or modify a specifically substituted thiophene. Although this book contains many references to the original literature, the large number of experimental recipes enables the user to prepare a thiophene derivative without access to the original literature. These features make the handbook especially useful for physicists working in material sciences and organic/pharmaceutical chemists, who rapidly want to find out the availability of (or how to make) a specific thiophene. - Contains a systematic description and critical evaluation of the best methods for preparation of thiophenes and polymers containing thiophenes - Rapid location of methods achieved by systematic division of substituents following the periodic table - All chapters are richly illustrated by detailed experimental proceedures for the synthesis of five membered heterocycles containing sulfur

HPLC for Pharmaceutical Scientists is an excellent book for both novice and experienced pharmaceutical chemists who regularly use HPLC as an analytical tool to solve challenging problems in the pharmaceutical industry. It provides a unified approach to HPLC with an equal and balanced treatment of the theory and practice of HPLC in the pharmaceutical industry. In-depth discussion of retention processes, modern HPLC separation theory, properties of stationary phases and columns are well blended with the practical aspects of fast and effective method development and method validation. Practical and pragmatic approaches and actual examples of effective development of selective and rugged HPLC methods from a physico-chemical point of view are provided. This book elucidates the role of HPLC throughout the entire drug development process from drug candidate inception to marketed drug product and gives detailed specifics of HPLC application in each stage of drug development. The latest advancements and trends in hyphenated and specialized HPLC techniques (LC-MS, LC-NMR, Preparative HPLC, High temperature HPLC, high pressure liquid chromatography) are also discussed.