Download or read book Linker Strategies in Solid Phase Organic Synthesis written by Peter Scott and published by John Wiley & Sons. This book was released on 2009-10-13 with total page 706 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Solid Phase Organic Synthesis written by Patrick H. Toy and published by John Wiley & Sons. This book was released on 2012-01-10 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Organic Synthesis on Solid Phase written by Florencio Zaragoza Dörwald and published by Wiley-VCH. This book was released on 2000-04-13 with total page 504 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Download or read book Solid Phase Peptide Synthesis written by Gregg B. Fields and published by Academic Press. This book was released on 1997-10-21 with total page 828 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Download or read book Solid Phase Organic Syntheses Volume 2 written by Peter J. H. Scott and published by John Wiley & Sons. This book was released on 2012-07-02 with total page 194 pages. Available in PDF, EPUB and Kindle. Book excerpt: Integrates solid-phase organic synthesis with palladium chemistry The Wiley Series on Solid-Phase Organic Syntheses keeps researchers current with major accomplishments in solid-phase organic synthesis, providing full experimental details. Following the validated, tested, and proven experimental procedures, readers can easily perform a broad range of complex syntheses needed for their own experiments and industrial applications. The series is conveniently organized into themed volumes according to the specific type of synthesis. This second volume in the series focuses on palladium chemistry in solid-phase synthesis, exploring palladium catalysts and reactions, procedures for preparation and utilization, ligands, and linker reactions. The first part of the volume offers a comprehensive overview of the field. Next, the chapters are organized into three parts: Part Two: Palladium-Mediated Solid-Phase Organic Syntheses Part Three: Immobilized Catalysts and Ligands Part Four: Palladium-Mediated Multifunctional Cleavage Each chapter is written by one or more leading international experts in palladium chemistry. Their contributions reflect a thorough examination and review of the current literature as well as their own first-hand laboratory experience. References at the end of each chapter serve as a gateway to the field's literature. The introduction of palladium-mediated, cross-coupling reactions more than thirty years ago revolutionized the science of carbon-carbon bond formation. It has now become a cornerstone of today's synthetic organic chemistry laboratory. With this volume, researchers in organic and medicinal chemistry have access to a single resource that explains the fundamentals of palladium chemistry in solid-phase synthesis and sets forth clear, step-by-step instructions for conducting their own syntheses.
Download or read book Solid Phase Organic Synthesis written by Patrick H. Toy and published by John Wiley & Sons. This book was released on 2012-01-18 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Biphasic Chemistry and The Solvent Case written by Jean-Philippe Goddard and published by John Wiley & Sons. This book was released on 2020-02-05 with total page 230 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Solid Phase Organic Synthesis written by Kevin Burgess and published by John Wiley & Sons. This book was released on 2004-04-05 with total page 294 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Solid Phase Organic Syntheses Volume 1 written by Anthony W. Czarnik and published by John Wiley & Sons. This book was released on 2004-04-07 with total page 176 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Stereoselective Synthesis of Drugs and Natural Products written by Vasyl Andrushko and published by John Wiley & Sons. This book was released on 2013-08-16 with total page 1836 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Sulfonyl Ynamides as Useful Tools for N Heterocyclic Chemistry written by Tim Wezeman and published by Logos Verlag Berlin GmbH. This book was released on 2016-12-31 with total page 253 pages. Available in PDF, EPUB and Kindle. Book excerpt: Sulfonyl ynamides are highly versatile and synthetically useful reagents. This thesis details the modular synthesis and use of sulfonyl ynamides in order to access N-heterocyclic scaffolds, such as quinolines and pyrazoles. The synthesis of a wide array of sulfonyl ynamides can be realized via copper-catalyzed amidative cross-couplings or by elimination of dichloroenamide precursors. Additionally the use of Sonogashira chemistry to further diversify terminal ynamides and the synthesis of solid-supported ynamides was investigated. Electrophilically-activated amides can be reacted with sulfonyl ynamides in order to access highly functionalized 4-aminoquinolines. The straightforward amide activation procedure with triflic anhydride and 2-chloropyridine was found to tolerate a wide range of substrates, which allowed for the development of a library of 4-aminoquinolines with ease. Moreover, 4-aminopyrazoles can be prepared by reacting terminal sulfonyl ynamides with sydnones under copper catalysis. However, as the copper catalysts were also found to promote the degradation of the ynamides, a copper-free strain-promoted alternative was developed. An in situ prepared 3-azacyclohexyne was found to tolerate a wide array of C-4 substituted sydnones, producing a mixture of both the 3,4- and 4,3-fused pyrazoles in good yields. Additional investigations into heterocyclic methodology led to the development of highly sophisticated, non-symmetrical and axially-chiral dibenzo-1,3-diazepines, -oxazepines and -thiazepines from simple, commercially available anilines. The anilines were coupled to their corresponding reaction partners via a chloromethyl intermediate and the 7-membered ring was subsequently formed using direct arylation.
Download or read book Combinatorial Chemistry written by Stephen R. Wilson and published by John Wiley & Sons. This book was released on 1997-03-28 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Peptide Synthesis and Applications written by Knud J. Jensen and published by Humana. This book was released on 2016-08-27 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Green Techniques for Organic Synthesis and Medicinal Chemistry written by Wei Zhang and published by John Wiley & Sons. This book was released on 2018-01-16 with total page 728 pages. Available in PDF, EPUB and Kindle. Book excerpt: An updated overview of the rapidly developing field of green techniques for organic synthesis and medicinal chemistry Green chemistry remains a high priority in modern organic synthesis and pharmaceutical R&D, with important environmental and economic implications. This book presents comprehensive coverage of green chemistry techniques for organic and medicinal chemistry applications, summarizing the available new technologies, analyzing each technique’s features and green chemistry characteristics, and providing examples to demonstrate applications for green organic synthesis and medicinal chemistry. The extensively revised edition of Green Techniques for Organic Synthesis and Medicinal Chemistry includes 7 entirely new chapters on topics including green chemistry and innovation, green chemistry metrics, green chemistry and biological drugs, and the business case for green chemistry in the generic pharmaceutical industry. It is divided into 4 parts. The first part introduces readers to the concepts of green chemistry and green engineering, global environmental regulations, green analytical chemistry, green solvents, and green chemistry metrics. The other three sections cover green catalysis, green synthetic techniques, and green techniques and strategies in the pharmaceutical industry. Includes more than 30% new and updated material—plus seven brand new chapters Edited by highly regarded experts in the field (Berkeley Cue is one of the fathers of Green Chemistry in Pharma) with backgrounds in academia and industry Brings together a team of international authors from academia, industry, government agencies, and consultancies (including John Warner, one of the founders of the field of Green Chemistry) Green Techniques for Organic Synthesis and Medicinal Chemistry, Second Edition is an essential resource on green chemistry technologies for academic researchers, R&D professionals, and students working in organic chemistry and medicinal chemistry.
Download or read book Drug Discovery Strategies and Methods written by Alexandros Makriyannis and published by CRC Press. This book was released on 2003-11-04 with total page 317 pages. Available in PDF, EPUB and Kindle. Book excerpt: Navigate the complex and multidisciplinary path of drug discovery procedures with Drug Discovery Strategies and Methods-a well-organized and timely reference that analyzes methods in target identification and validation, lead detection, compound optimization, and biological testing. This volume addresses challenges encountered during the discovery of new pharmaceutical candidates including the use of cutting-edge techniques utilized in drug design and development. It considers key elements in the drug design cycle ranging from appropriateness of targets and disease models to compound characterization, safety, and efficacy and the role of protein crystallography in structure-based drug design.
Download or read book Small Molecule Medicinal Chemistry written by Werngard Czechtizky and published by John Wiley & Sons. This book was released on 2015-09-25 with total page 528 pages. Available in PDF, EPUB and Kindle. Book excerpt: Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting
Download or read book Solid supported Combinatorial and Parallel Synthesis of Small molecular weight Compound Libraries written by D. Obrecht and published by Elsevier. This book was released on 1998-10-16 with total page 366 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book gives an overview of the current state of the art of combinatorial organic synthesis. While the main focus is on multicomponent and multigeneration strategies using polymeric supports, there is also a Chapter on solution strategies using polymer-grafted reagents which allow minimisation of work-up procedures. Some of the most important strategies and tools are presented and summarised, with an explanation of the pivotal role of organic synthesis in the creation of diversity.
