Über die Autorin bzw. den Autor

PIERFAUSTO SENECI, PhD, is Associate Director of Chemistry at the Glaxo Wellcome Medicines Research Centre, Verona, Italy.

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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

Aus dem Klappentext

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

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SOLID-PHASE SYNTHESIS AND COMBINATORIAL TECHNOLOGIES

JOHN WILEY & SONS, INC.

Contents

Preface................................................................................................................................................ix1 Solid-Phase Synthesis: Basic Principles..............................................................................................................11.1 Solid Supports.....................................................................................................................................11.2 Linkers............................................................................................................................................91.3 Reaction Monitoring in Solid-Phase Synthesis.......................................................................................................261.4 Purity and Yield Determination in Solid-Phase Synthesis............................................................................................33References.............................................................................................................................................382 Solid-Phase Synthesis: Oligomeric Molecules..........................................................................................................452.1 Peptides...........................................................................................................................................452.2 Oligonucleotides...................................................................................................................................572.3 Oligosaccharides...................................................................................................................................71References.............................................................................................................................................843 Solid-Phase Synthesis: Small Organic Molecules.......................................................................................................913.1 Small Organic Molecules on Solid Phase: Target Selection and Solution Studies......................................................................923.2 Small Organic Molecules on Solid Phase: Solid-Phase Synthesis......................................................................................933.3 Small Organic Molecules on Solid Phase: From Solid-Phase Synthesis to Synthetic Organic Libraries..................................................963.4 An Example: Solid-Phase Synthesis of 1H-[2]Pyrindinones............................................................................................983.5 Solid-Phase Synthetic Strategies: Selected Examples................................................................................................107References.............................................................................................................................................1344 Combinatorial Technologies: Basic Principles.........................................................................................................1364.1 Combinatorial Technologies.........................................................................................................................1364.2 Combinatorial Libraries............................................................................................................................142References.............................................................................................................................................1625 Synthetic Organic Libraries: Library Design and Properties...........................................................................................1655.1 Primary Libraries: Shooting in the Dark?...........................................................................................................1655.2 Focused Libraries: High-Throughput Structure-Activity Relationships................................................................................1705.3 Biased-Targeted Libraries: Information-Rich Primary Libraries......................................................................................1745.4 Library Design via Computational Tools.............................................................................................................176References.............................................................................................................................................2046 Synthetic Organic Libraries: Solid-Phase Discrete Libraries..........................................................................................2106.1 Synthesis of Solid-Phase Discrete Libraries........................................................................................................2106.2 Structure Determination, Quality Control, and Purification of Solid-Phase Discrete Libraries.......................................................2156.3 Examples of Solid-Phase Discrete Library Synthesis.................................................................................................2246.4 New Trends in Solid-Phase Discrete Library Synthesis...............................................................................................246References.............................................................................................................................................2557 Synthetic Organic Libraries: Solid-Phase Pool Libraries..............................................................................................2647.1 Synthesis of Solid-Phase Pool Libraries............................................................................................................2647.2 Direct Structure Determination of Positives from Solid-Phase Pool Libraries........................................................................2797.3 Deconvolution Methods for Solid-Phase Pool Libraries...............................................................................................2907.4 Encoding Methods for Solid-Phase Pool Libraries....................................................................................................3017.5 New Trends in Solid-Phase Pool Libraries...........................................................................................................318References.............................................................................................................................................3288 Synthetic Organic Libraries: Solution-Phase Libraries................................................................................................3398.1 Solution- Versus Solid-Phase Synthetic Libraries: Which Ones to Use?...............................................................................3398.2 Solution-Phase Discrete Libraries..................................................................................................................3468.3 Purification of Solution-Phase Library Intermediates and Final Compounds: LiquidLiquid and Solid-Phase Extraction Systems.....................3618.4 Solid-Phase Assisted Solution-Phase Library Synthesis and Purification.............................................................................3728.5 Soluble Supports in Solution-Phase Combinatorial Synthesis.........................................................................................3978.6 New Trends in Solution-Phase Combinatorial...