Linker Strategies in Solid-Phase Organic Synthesis


Book Description

Linker design is an expanding field with an exciting future in state-of-the-art organic synthesis. Ever-increasing numbers of ambitious solution phase reactions are being adapted for solid-phase organic chemistry and to accommodate them, large numbers of sophisticated linker units have been developed and are now routinely employed in solid-phase synthesis. Linker Strategies in Solid-Phase Organic Synthesis guides the reader through the evolution of linker units from their genesis in solid-supported peptide chemistry to the cutting edge diversity linker units that are defining a new era of solid phase synthesis. Individual linker classes are covered in easy to follow chapters written by international experts in their respective fields and offer a comprehensive guide to linker technology whilst simultaneously serving as a handbook of synthetic transformations now possible on solid supports. Topics include: the principles of solid phase organic synthesis electrophile and nucleophile cleavable linker units cyclative cleavage as a solid phase strategy photocleavable linker units safety-catch linker units enzyme cleavable linker units T1 and T2 –versatile triazene linker groups hydrazone linker units benzotriazole linker units phosphorus linker units sulfur linker units selenium and tellurium linker units sulfur, oxygen and selenium linker units cleaved by radical processes silicon and germanium linker units boron and stannane linker units bismuth linker units transition metal carbonyl linker units linkers releasing olefins or cycloolefins by ring-closing metathesis fluorous linker units solid-phase radiochemistry The book concludes with extensive linker selection tables, cataloguing the linker units described in this book according to the substrate liberated upon cleavage and conditions used to achieve such cleavage, enabling readers to choose the right linker unit for their synthesis. Linker Strategies in Solid-Phase Organic Synthesis is an essential guide to the diversity of linker units for organic chemists in academia and industry working in the broad areas of solid-phase organic synthesis and diversity oriented synthesis, medicinal chemists in the pharmaceutical industry who routinely employ solid-phase chemistry in the drug discovery business, and advanced undergraduates, postgraduates, and organic chemists with an interest in leading-edge developments in their field.




Solid-Phase Organic Synthesis


Book Description

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.




Solid-Phase Peptide Synthesis


Book Description

The critically acclaimed laboratory standard for more than forty years, Methods in Enzymology is one of the most highly respected publications in the field of biochemistry. Since 1955, each volumehas been eagerly awaited, frequently consulted, and praised by researchers and reviewers alike. More than 275 volumes have been published (all of them still in print) and much of the material is relevant even today-truly an essential publication for researchers in all fields of life sciences. Key Features * Solid-phase peptide synthesis * Applications of peptides for structural and biological studies * Characterization of synthetic peptides




Biphasic Chemistry and The Solvent Case


Book Description

Biphasic Chemistry and The Solvent Case examines recent improvements in reaction conditions, in order to affirm the role of chemistry in the sustainable field. This book shows that those who work within the chemistry industry support limits for the use of toxic or flammable solvents, since it reduces the purifications to simple filtrations. Thanks to commercial scavengers, solid phase syntheses are now available to all. Fluorine biphasic catalysis enables extremely efficient catalyst recycling and has a high applicability potential at the industrial level. This book also reviews the many studies that have shown that water is a solvent of choice for most synthetic reactions. Particular traits can be obtained and the effects on thermodynamics make it possible to operate at lower temperatures, thereby achieving energy savings. Finally the great diversity of application of the reactions without solvents is illustrated.




Solid-Phase Organic Synthesis


Book Description

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.




Solid-Phase Organic Syntheses, Volume 1


Book Description

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.




Peptide Synthesis and Applications


Book Description

Peptides are used ubiquitously for studies in biology, biochemistry, chemical biology, peptide based medicinal chemistry, and many other areas of research. There is a number of marketed peptide drugs, and the prospects for the development of new peptide drugs are very encouraging. The second edition of Peptide Synthesis and Applications expands upon the previous editions with current, detailed methodologies for peptide synthesis. With new chapters on laboratory protocols for both the specialist and the non-specialist. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Peptide Synthesis and Application, Second Edition seeks to aid scientists in understanding different approaches to the synthesis of peptides by using a broad range of methods and strategies.




Electrochemistry in Nonaqueous Solutions


Book Description

Nonaqueous solutions are equally indispensable to electrochemistry. Here, Kosuke Izutsu brilliantly illustrates the numerous aspects of this fascinating topic, whether the focus be on physicochemical processes or analytical methods. The author discusses solvation and solvent effects emphasizing dynamic aspects, important reactions including ionic and supercritical media, as well as advanced techniques in polarography and voltammetry. Throughout, he effortlessly manages to provide a comprehensive overview while also presenting the very latest developments. A number of example applications further enhance the practical value of this book and give it the feel of a reference work. Written for both users and specialists this volume represents a wealth of vital information and belongs on every bookshelf.




Fmoc Solid Phase Peptide Synthesis


Book Description

Since the publication of Atherton and Sheppard's volume, the technique of Fmoc solid-phase peptide synthesis has matured considerably and is now the standard approach for the routine production of peptides. The focus of this new volume is much broader, and covers the essential procedures.




Stereoselective Synthesis of Drugs and Natural Products


Book Description

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.