Revised, and updated Design and Optimization in Organic Synthesis presents strategies to explore experimental conditions and methodologies for systematic studies of entire reaction systems (substrates, reagent(s), catalyst(s), and solvents). Chemical phenomena are not usually the result of a single factor and this book describes how statistically designed methods can be used to analyse and evaluate synthetic procedures. The methodology is based on multivariate statistical techniques. The accompanying CD contains data tables and programmes. This book is essential reading for anyone working in process design and development in fine chemicals or the pharmaceutical industry, and is suitable for those with no experience in the field. * Contains recalculated models and redrawn figures, as well as new chapters on for example, the design of combinatorial libraries * Presents strategies to explore experimental conditions and methodologies * Enables the analysis and prediction of the best synthetic procedures

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.

This is the first general textbook on experimental design and optimization in organic synthesis. The book presents a unified methodology for carrying out systematic studies when the objective is to develop efficient and optimum synthetic methods. Strategies are included both for exploring the experimental conditions and for systematic studies of entire reaction systems (substrates, reagent(s) and solvents). The methodology is based on multivariate statistical techniques. The following topics are treated in depth: classical two-level designs for screening experiments, gradient methods (steepest ascent, simplex methods) as well as response surface techniques for optimization, principal components analysis and PLS modelling. The book is intended as a hands-on text for chemists and engineers engaged in developing synthetic methods in industrial research, e.g. in fine chemicals and pharmaceuticals production, as well as for advanced undergraduate students, graduate students, and researchers in an academic environment.

Presents both the fundamental concepts and the most recent applications in solid-phase organic synthesis With its emphasis on basic concepts, Solid-Phase Organic Synthesis guides readers through all the steps needed to design and perform successful solid-phase organic syntheses. The authors focus on the fundamentals of heterogeneous supports in the synthesis of organic molecules, explaining the use of a solid material to facilitate organic synthesis. This comprehensive text not only presents the fundamentals, but also reviews the most recent research findings and applications, offering readers everything needed to conduct their own state-of-the-art science experiments. Featuring chapters written by leading researchers in the field, Solid-Phase Organic Synthesis is divided into two parts: Part One, Concepts and Strategies, discusses the linker groups used to attach the synthesis substrate to the solid support, colorimetric tests to identify the presence of functional groups, combinatorial synthesis, and diversity-oriented synthesis. Readers will discover how solid-phase synthesis is currently used to facilitate the discovery of new molecular functionality. The final chapter discusses how using a support can change or increase reaction selectivity. Part Two, Applications, presents examples of the solid-phase synthesis of various classes of organic molecules. Chapters explore general asymmetric synthesis on a support, strategies for heterocyclic synthesis, and synthesis of radioactive organic molecules, dyes, dendrimers, and oligosaccharides. Each chapter ends with a set of conclusions that underscore the key concepts and methods. References in each chapter enable readers to investigate any topic in greater depth. With its presentation of basic concepts as well as recent findings and applications, Solid-Phase Organic Synthesis is the ideal starting point for students and researchers in organic, medicinal, and combinatorial chemistry who want to take full advantage of current solid-phase synthesis techniques.

The rapid expansion of combinatorial chemistry has renewed interest in solid-phase organic synthesis, a method that lends itself well to creating and screening large numbers of lead compounds. Solid-Phase Organic Syntheses, Volume 1 is the first volume in a series that will be updated annually, filling a gap in the existing chemical literature. Providing information previously unavailable from a single resource, this series is dedicated to providing researchers in the field with validated and tested methods for the solid-phase synthesis of interesting and biologically relevant molecules. Solid-phase methods will virtually always be invented for application in combinatorial organic synthesis. To meet these specific needs, Solid-Phase Organic Syntheses, Volume 1 focuses on a single type of synthetic transformation accomplished on solid support, and indicates how procedures are optimized to work with a structurally-wide variety of reagents. Written by recognized leaders in the field who review and test all chemical protocols before publication, organic transformations are organized by type of compound synthesized and reaction type. For the first time, experimental details for proven solid-phase synthetic molecules are collected in a single, invaluable resource. Solid-Phase Organic Syntheses, Volume 1 provides combinatorial chemists and researchers in organic chemistry and medicinal chemistry with the tools and descriptive protocols to achieve syntheses of desired compounds using a variety of solid supports and reagents.