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.

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.

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.

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

Good methods must be reliable, well-tested, and honed to minimize the time and expense required to achieve the desired results. CPNC provides a continuously growing and evolving set of protocols that allows researchers to benefit from the experience of other researchers around the world. The core manual provides a comprehensive set of protocols that have been compiled, revised, and streamlined over the last 6 years. Quarterly updates provide new protocols in emerging areas of research as well as continued advances and new applications for fundamental methods. The book is designed to grow and change with the field of nucleic acid chemistry. Fundamental nucleoside chemistry methods include sugar-base condensation, phosphorylation, and nucleoside protection. Methods for oligonucleotide synthesis include H-phosphonate and phosphoramidite approaches, solid-phase and solution-phase synthesis, large-scale synthesis, synthesis for modified and unmodified oligonucleotides, conjugation of oligonucleotides, synthesis without base protection, and synthesis on microarrays. More specialized synthetic methods include synthesis of biologically active nucleosides and prodrugs. Purification and characterization methods are detailed. Advanced methods include biophysical analysis, combinatorial methods, and nanotechnology. Each protocol includes rationale for choosing appropriate methods, step-by-step procedures, complete recipes, anticipated results, characterization data, and troubleshooting, as well as background and recommended reading. The level of procedural detail is far beyond that found in the research literature, and tips and comments from authors are geared towards ensuring reliable duplication in the laboratory.

The new time-saving revolution in drug discovery. Combinatorial chemistry, a method for synthesizing millions of chemical compounds much faster than usual, is becoming one of the most useful technical tools available to chemists and researchers working today. Using current advances in computer and laboratory techniques, combinatorial chemistry has freed professionals from the drudgery of piecemeal experimental work and opened new creative possibilities for experimentation. Combinatorial Chemistry: Synthesis and Application details critical aspects of the technique, featuring the work of some of the world's leading chemists, many of whom played a key role in its development. Including examples of both solution-phase and solid-phase approaches as well as the full complement of organic chemistry technologies currently available, the book describes: * Concepts and terms of combinatorial chemistry * Polymer-supported synthesis of organic compounds * Macro beads as microreactors * Solid-phase methods in combinatorial chemistry * Encoded combinatorial libraries, including Rf-encoding of synthesis beads * Strategies for combinatorial libraries of oligosaccharides * Combinatorial libraries of peptides, proteins, and antibodies using biological systems. While combinatorial chemistry originated in peptide chemistry, this volume has deliberately focused on nonpeptide organic applications, illustrating the technique's wide uses. Combinatorial Chemistry introduces organic, medicinal, and pharmaceutical chemists as well as biochemists to this exciting, cost-effective, and practical technique, which has unlocked creative potential for the next millennium.

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.