The complexity of natural products and the inherent challenges imposed by target synthesis were used as a platform to develop new strategies and linkers for solid phase organic synthesis. This research led to the development of two cyclorelease reaction involving an olefin metathesis and a Stille reaction. Our interest in linkers also led to the development of three new linkers; a simplified photolabile linker, a very versatile selenium linker and a new safety-catch linker. The utility of these developments were illustrated by the solid phase synthesis of heptasaccharide phytoalexin elicitor (HPE), epothilone A, zearalenone, sarcodictyins and vancomycin (Figure 1). Libraries of the promising anticancer agents epothilone and sarcodictyins provided valuable information towards the structure-activity relationship of these molecules as well as several compounds with improved biological activity.

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.

This is the number–one successful book on solid phase organic synthesis, now in its second, expanded edition. It offers the reader · a comprehensive overview of supports, spacers, and linkers · 15% more contents · everything there is to know about reactions and their applications · clear structure · numerous experimental guidelines for use in practice The ideal reference for newcomers and experts. "... I have no doubts that this text will be the benchmark for future publications on the subject, and a very hard act to follow for authors planning books of their own on this red hot topic." The Alchemist

Brings together the best tested and proven stereoselective synthetic methods Both the chemical and pharmaceutical industries are increasingly dependent on stereoselective synthetic methods and strategies for the generation of new chiral drugs and natural products that offer specific 3-D structures. With the publication of Stereoselective Synthesis of Drugs and Natural Products, researchers can turn to this comprehensive two-volume work to guide them through all the core methods for the synthesis of chiral drugs and natural products. Stereoselective Synthesis of Drugs and Natural Products features contributions from an international team of synthetic chemists and pharmaceutical and natural product researchers. These authors have reviewed the tremendous body of literature in the field in order to compile a set of reliable, tested, and proven methods alongside step-by-step guidance. This practical resource not only explores synthetic methodology, but also reaction mechanisms and applications in medicinal chemistry and drug discovery. The publication begins with an introductory chapter covering general principles and methodologies, nomenclature, and strategies of stereoselective synthesis. Next, it is divided into three parts: Part One: General Methods and Strategies Part Two: Stereoselective Synthesis by Bond Formation including C-C bond formation C-H bond formation C-O bond formation C-N bond formation Other C-heteroatom formation and other bond formation Part Three: Methods of Analysis and Chiral Separation References in every chapter serve as a gateway to the literature in the field. With this publication as their guide, chemists involved in the stereoselective synthesis of drugs and natural products now have a single, expertly edited source for all the methods they need.

Here, H.-G. Schmalz and T. Wirth have put together a collection of current contributions on the most important topics in organic chemistry all in one handy book. Like its successful predecessors, this volume provides readers with numerous articles on the current state of synthetic methods and their applications. The wide range covered by nearly forty contributions ensures a concise overview of the latest developments in the field, whether they be new methods of C-C bond formation or racemization, asymmetric phase-transfer catalysis or stereoselective metathesis reactions, solid phase reactions or particularly elegant syntheses of challenging natural products. Throughout, the highly renowned authors guarantee the exceptionally high quality of the articles, making this an indispensable read for everyone wanting to stay abreast of developments in organic chemistry.

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.