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Optimization of Solid-Phase Combinatorial Synthesis

Optimization of Solid-Phase Combinatorial Synthesis
Author: Bing Yan
Publisher: CRC Press
Total Pages: 408
Release: 2001-12-04
Genre: Science
ISBN: 1482271052

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"Addresses the key topic in combinatorial synthesis--how to optimize the quality of a combinatorial library--by determining the usefulness of synthesized compunds, the reliability of biological assay results, and analyzing acadmic and industrial applications, real-world examples, and case studies of successful and unsuccessful technologies."


Solid-Phase Organic Synthesis

Solid-Phase Organic Synthesis
Author: Kevin Burgess
Publisher: John Wiley & Sons
Total Pages: 294
Release: 2004-04-05
Genre: Science
ISBN: 0471458457

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Solid-Phase Organic Synthesis Edited by Kevin Burgess, Texas A & M University Efficient, high-throughput chemistry is now the focus of many research laboratories. Solid-phase organic syntheses are central to many of these combinatorial and parallel screening methodologies. Consequently, they have been a major scientific theme of the 1990s and promise to remain prominent for the first part of the new millennium. Indeed, a bewildering number of papers have entered the literature on this topic; some report minor modifications enabling transformation of solution-phase methods to a solid support, while others report major innovations. Solid-Phase Organic Synthesis collects, highlights, and critiques some of the key developments in the field. Leading practitioners explain different perspectives on diverse aspects of the area. Specific topics covered include: * Syntheses of guanidines * Palladium-catalyzed C-C bond forming reactions * S_nAr reactions for the formation of heterocycles * Sequence-specific arylalkyne oligomers * Resin-supported capture agents and other reagents * Synthesis on pins * Monitoring of supported reactions using IR * Solid-phase syntheses of natural product derivatives Of related interest . Combinatorial Chemistry and Molecular Diversity in Drug Discovery Eric M. Gordon and James F. Kerwin 1998 (0-471-15518-7) 544 pp. Combinatorial Chemistry Synthesis and Application Stephen R. Wilson and Anthony W. Czarnik 1997 (0-471-12687-X) 288 pp.


Solid-Phase Synthesis and Combinatorial Technologies

Solid-Phase Synthesis and Combinatorial Technologies
Author: Pierfausto Seneci
Publisher: John Wiley & Sons
Total Pages: 653
Release: 2003-05-28
Genre: Science
ISBN: 0471460737

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A unique, integrated look at solid-phase synthesis and advances in combinatorial chemistry and technologies The last decade has seen a rapid expansion in combinatorial technologies, a field where chemistry disciplines intersect with automation, statistics, and information science, as well as certain biological disciplines. Reflecting these multidisciplinary trends, this new work provides a comprehensive overview of the most important aspects of solid-phase synthesis (SPS), combinatorial chemistry, and related combinatorial technologies. It clearly demonstrates how SPS and combinatorial chemistry have extended their application from the pharmaceutical arena to new areas, including biotechnology, material sciences, catalysis, and agrochemical industries, and explores in detail strategies for planning, designing, preparing, and testing of combinatorial libraries in various disciplines. Designed to meet the needs of both experienced combinatorial chemists and newcomers to the field, Solid-Phase Synthesis and Combinatorial Technologies: * Surveys the most recent developments in SPS and combinatorial chemistry * Explains the entire process, from determining the need for a library to the details necessary for synthesis of the library * Discusses choice of format, size, and the rationale behind the design of each synthetic step * Surveys the analytical techniques and the purification methods used to characterize and purify combinatorial libraries * Employs a large number of examples to illustrate important concepts * Includes problems geared toward applying acquired knowledge and designing the steps to SPS/library synthesis * Describes the quality control and activity screening of combinatorial libraries for various applications * Features a detailed bibliography of more than 1,700 relevant sources


Combinatorial Library

Combinatorial Library
Author: Lisa B. English
Publisher: Springer Science & Business Media
Total Pages: 380
Release: 2008-02-04
Genre: Science
ISBN: 1592592856

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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.