Domino Reactions in Drug Discovery presents a concise selection of domino reactions employed in routes for the synthesis of pharmaceuticals, agrochemicals and the design of new drug candidates. These versatile reactions play an important and integral part in both the aesthetic appeal and functional aspects of strategic drug discovery, lending enhanced efficiency and synthetic versatility to pharmaceutical drug design. Due to their atom economy, these reactions are increasingly popular in the development of complex scaffolds and multifunctional derivatives aimed at the synthesis of new chemical entities and approved APIs across diverse therapeutic classes, including antidiabetics [DPP4 inhibitors], anticancer therapies and HIV integrase inhibitors. Features illustrated schemes with mechanisms, procedures and results Includes a compendium of Domino Name Reactions for drugs Provides a concise, comprehensive coverage of domino reactions in drug discovery, with a focus on sustainable practices
Domino reactions enable you to build complex structures in one-pot reactions without the need to isolate intermediates- a dream comes true. In this book, the well-respected expert, Professor Lutz Tietze, summarizes the possibilities of this reaction type - an approach for an efficiant, economically benificial and ecological benign synthesis. A definite must for every organic chemist.
The follow-up to the successful "Domino Reaction in Organic Synthesis", this ready reference brings up to date on the original concept. The chapters have been arranged according to the name of well-known transformations of the first step and in combination with the formed products. Each chapter is written by an internationally renowned expert, and the book is edited by L. F. Tietze, who established the concept of domino reactions. The one-stop source for all synthetic chemists to improve the synthetic efficiency and allow an ecologically and economically beneficial preparation of every chemical compound.
This book covers the latest developments in asymmetric domino reactions, focussing on those published in the last 6 years. These fascinating reactions have rapidly become one of the most current fields in organic chemistry, since they allow reaching easily high molecular complexity in an economically favourable way with advantages of savings in solvent, time, energy, and costs. Unsurprisingly, the high levels of efficiency and enantioselectivity generally reached in these reactions have been exploited for the production of a wide number of complex chiral molecules with dense stereochemistry and functionality, which are motifs present in biologically active compounds and natural products. The book is divided into three principal sections, dealing successively with asymmetric domino reactions based on the use of chiral auxiliaries, asymmetric domino reactions based on the use of chiral metal catalysts, and asymmetric domino reactions based on the use of chiral organocatalysts, covering the literature since the beginning of 2006.
A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.
Discover an enhanced synthetic approach to developing andscreening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developinglarge collections of structurally diverse small molecules as probesto investigate biological pathways. This book presents the mosteffective methods in diversity-oriented synthesis for creatingsmall molecule collections. It offers tested and proven strategiesfor developing diversity-oriented synthetic libraries and screeningmethods for identifying ligands. Lastly, it explores some promisingnew applications based on diversity-oriented synthesis that havethe potential to dramatically advance studies in drug discovery andchemical biology. Diversity-Oriented Synthesis begins with an introductorychapter that explores the basics, including a discussion of therelationship between diversity-oriented synthesis and classiccombinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of smallmolecules using diversity-oriented principles, includingpeptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis bydescribing chemical libraries Provides modern approaches to screening diversity-orientedsynthetic libraries, including high-throughput and high-contentscreening, small molecule microarrays, and smart screeningassays Presents the applications of diversity-oriented syntheticlibraries and small molecules in drug discovery and chemicalbiology, reporting the results of key studies and forecasting therole of diversity-oriented synthesis in future biomedicalresearch This book has been written and edited by leading internationalexperts in organic synthesis and its applications. Theircontributions are based on a thorough review of the currentliterature as well as their own firsthand experience developingsynthetic methods and applications. Clearly written and extensively referenced,Diversity-Oriented Synthesis introduces novices to thishighly promising field of research and serves as a springboard forexperts to advance their own research studies and develop newapplications.
Demonstrates the advantages of catalytic cascade reactionsfor synthesizing natural products and pharmaceuticals Riding the wave of green chemistry, catalytic cascade reactionshave become one of the most active research areas in organicsynthesis. During a cascade reaction, just one reaction solvent,one workup procedure, and one purification step are needed, thussignificantly increasing synthetic efficiency. Featuring contributions from an international team of pioneersin the field, Catalytic Cascade Reactions demonstrates theversatility and application of these reactions for synthesizingvaluable compounds. The book examines both organocatalysis andtransition-metal catalysis reactions, bringing readers up to datewith the latest discoveries and activities in all major areas ofcatalytic cascade reaction research. Catalytic Cascade Reactions begins with three chaptersdedicated to organocatalytic cascade reactions, exploring amines,Brønsted acids, and the application of organocatalytic cascadereactions in natural product synthesis and drug discovery. Next,the book covers: Gold-catalyzed cascade reactions Cascade reactions catalyzed by ruthenium, iron, iridium,rhodium, and copper Palladium-catalyzed cascade reactions of alkenes, alkynes, andallenes Application of transition-metal catalyzed cascade reactions innatural product synthesis and drug discovery Engineering mono- and multifunctional nanocatalysts for cascadereactions Multiple-catalyst-promoted cascade reactions All chapters are thoroughly referenced, providing quick accessto important original research findings and reviews so that readerscan explore individual topics in greater depth. Drawing together and analyzing published findings scatteredacross the literature, this book provides a single source thatencapsulates our current understanding of catalytic cascadeprocesses. Moreover, it sets the stage for the development of newcatalytic cascade reactions and their applications.
Retaining the proven didactic concept of the successful "Chemical Biology - Learning through Case Studies", this sequel features 27 new case studies, reflecting the rapid growth in this interdisciplinary topic over the past few years. Edited by two of the world's leading researchers in the field, this textbook introduces students and researchers to the modern approaches in chemical biology, as well as important results, and the techniques and methods applied. Each chapter presents a different biological problem taken from everyday lab work, elucidated by an international team of renowned scientists. With its broad coverage, this is a valuable source of information for students, graduate students, and researchers working on the borderline between chemistry, biology, and biochemistry.
In the very first book on this hot topic, the expert editors andauthors present a comprehensive overview of these elegantreactions. From the contents: Organoboron compounds Free-radical mediated multicomponent coupling reactions Applications in drug discovery Metal catalyzed reactions Total synthesis of natural products Asymmetric isocyanide-based reactions The Biginelli reaction Asymmetric isocyanide-based reactions The Domino-Knoevenagel-Hetero-Diels-Alder Reaction and relatedtransformations Catalytic asymmetric reactions Algorithm based methods for discovering novel reactions Post-condensation modifications of the Passerini and Ugireactions An essential reference for organic and catalytic chemists, andthose working in organometallics both in academia and industry.
This volume of Pharmacochemistry Library comprises the text of invited lectures presented at the 11th Noordwijkerhout-Camerino Symposium Trends in Drug Research, held in Noordwijkerhout, The Netherlands, from 11-15 May 1997. In the programme attention has been given to the generation of new biological target systems and the generation of new lead molecules, with presentations on e.g. combinatorial chemistry, compound libraries, database search, high throughput screening and molecular biology. Other topics discussed were the perspectives for new medicines for the gastro-intestinal tract, the major developments in the search for effective anti-HIV drugs and new aspects in synthetic approaches. In a special session three topics which currently draw much attention were discussed: How to deal with the major problem of resistance against antimirobial agents? Can the apoptosis mechanism be used as a drug target? Is the newly observed phenomenon of inverse agonism a general principle and has it consequences for drug development (and use?)
This two-colored textbook presents not only synthetic ways to design organic compounds, it also contains a compilation of the most important total synthesis of the last 50 years with a comparative view of multiple designs for the same targets. It explains different tactics and strategies, making it easy to apply to many problems, regardless of the synthetic question in hand. Following a historical view of the evolution of synthesis, the book goes on to look at principles and issues impacting synthesis and design as well as principles and issues of methods. The sections on comparative design cover classics in terpenes and alkaloid synthesis, while a further section covers such miscellaneous syntheses as Maytansine, Palytoxin, Brevetoxin B and Indinavir. The whole is rounded off with a look at future perspectives and, what makes this textbook extraordinairy, with personal recollections of the chemists, who synthesized these fascinating compounds. With its attractive layout highlighting key parts and tactics using a second color, this is a useful tool for organic chemists, lecturers and students in chemistry, as well as those working in the chemical industry. "I think, as will many organic chemists, that the Hudlicky book will be the Bible of synthetic organic chemistry, the past, the present and the future. A hallmark publication." (Victor Snieckus)
The second edition of Comprehensive Organic Synthesis—winner of the 2015 PROSE Award for Multivolume Reference/Science from the Association of American Publishers—builds upon the highly respected first edition in drawing together the new common themes that underlie the many disparate areas of organic chemistry. These themes support effective and efficient synthetic strategies, thus providing a comprehensive overview of this important discipline. Fully revised and updated, this new set forms an essential reference work for all those seeking information on the solution of synthetic problems, whether they are experienced practitioners or chemists whose major interests lie outside organic synthesis. In addition, synthetic chemists requiring the essential facts in new areas, as well as students completely new to the field, will find Comprehensive Organic Synthesis, Second Edition an invaluable source, providing an authoritative overview of core concepts. Winner of the 2015 PROSE Award for Multivolume Reference/Science from the Association of American Publishers Contains more than170 articles across nine volumes, including detailed analysis of core topics such as bonds, oxidation, and reduction Includes more than10,000 schemes and images Fully revised and updated; important growth areas—including combinatorial chemistry, new technological, industrial, and green chemistry developments—are covered extensively
Reports progress on chemical, enzymatic, phage, and cell-derived libraries. Discusses synergy between structure-based design and combinatorial libraries. Presents applications of combinatorial libraries to drug discovery and new synthetic catalysis. Reports library screening approaches, including the use of NMR. Presents recent advances in solid-phase organic synthesis, liquid-phase organic synthesis, and high-throughput combinatorial organic synthesis. Discusses automation of organic synthesis as well as new methodologies for monitoring solid-phase organic synthesis.
|Author||: Zbigniew J. Witczak,Roman Bielski|
|Publisher||: John Wiley & Sons|
|Release Date||: 2016-02-23|
|ISBN 10||: 1119044200|
|Pages||: 368 pages|
The book consists of a brief introduction, a foreward provided by professor Danishefsky of Columbia University, and about 14 – 16 chapters, each written by one or two eminent scholars/authors describing their recent research in the area of either domino reactions or intramolecular rearrangements in carbohydrate chemistry. Three or four chapters will be reviews. The domino (cascade, tandem) reactions are always intramolecular. They are usually very fast, clean and offer highly complex structures in a one pot process. Intramolecular rearrangements offer very similar advantages and often lead to highly complex products as well. Although many recently isolated carbohydrates fulfill various sophisticated functions, their structures are often very complex. The editors cover the broadest scope of novel methodologies possible. All the synthetic and application aspects of domino/cascade reactions are explored in this book. A second theme that will be covered is intramolecular rearrangement, which is also fast, stereoselective, and often constitutes one or more steps of domino /cascade process. Selected examples of intramolecular rearrangements are presented. Together, both processes offer an elegant and convenient approach to the synthesis of many complex molecules, which are normally difficult to synthesize via alternative routes. It appears that domino and intramolecular rearrangements are ideally suited to synthesize certain specific modified monosaccharides. What is particularly important is that both processes are intermolecular and almost always yield products with very well-defined stereochemistry. This high definition is absolutely crucial when synthesizing advanced, modified mono and oligosaccharides. The choice of contributors reflects an emphasis on both therapeutic and pharmacological aspects of carbohydrate chemistry.
Although many books exist on the subject of chiral chemistry, they only briefly cover chiral synthesis and analysis as a minor part of a larger work, to date there are none that pull together the background information and latest advances in one comprehensive reference work. Comprehensive Chirality provides a complete overview of the field, and includes chiral research relevant to synthesis, analytic chemistry, catalysis, and pharmaceuticals. The individual chapters in each of the 9 volumes provide an in depth review and collection of references on definition, technology, applications and a guide/links to the related literature. Whether in an Academic or Corporate setting, these chapters will form an invaluable resource for advanced students/researchers new to an area and those who need further background or answers to a particular problem, particularly in the development of drugs. Chirality research today is a central theme in chemistry and biology and is growing in importance across a number of disciplinary boundaries. These studies do not always share a unique identifying factor or subject themselves to clear and concise definitions. This work unites the different areas of research and allows anyone working or researching in chiral chemistry to navigate through the most essential concepts with ease, saving them time and vastly improving their understanding. The field of chirality counts several journals that are directly and indirectly concerned with the field. There is no reference work that encompasses the entire field and unites the different areas of research through deep foundational reviews. Comprehensive Chirality fills this vacuum, and can be considered the definitive work. It will help users apply context to the diverse journal literature offering and aid them in identifying areas for further research and/or for solving problems. Chief Editors, Hisashi Yamamoto (University of Chicago) and Erick Carreira (ETH Zürich) have assembled an impressive, world-class team of Volume Editors and Contributing Authors. Each chapter has been painstakingly reviewed and checked for consistent high quality. The result is an authoritative overview which ties the literature together and provides the user with a reliable background information and citation resource.
Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. Presents information in a clear and concise way using a large number of figures Historical background provides insights on how the process of drug discovery in the anticancer field has evolved Extensive references to primary literature
Antitumor chemotherapy is nowadays a very active field of research, and a huge amount of information on the topic is generated every year. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book addresses the need for an updated treatment from the point of view of medicinal chemistry and drug design. The focus of Medicinal Chemistry of Anticancer Drugs is on the mechanism of action of antitumor drugs from the molecular point of view and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents, aiming at the rationalization of the action of this type of drug, which would allow the design of new active structures. * Explains the biological basis of cancer treatment and the role of chemists in improving anticancer drugs * Provides the historical background and serves as a comprehensive and practical guide on cancer research and anticancer drug development * Includes coverage of different approaches to treating cancer, drug resistance, and a chapter on cancer prevention
Classics in Total Synthesis II is the long awaited sequel to Classics in Total Synthesis, a book that has made its mark as a superb tool for educating students and practitioners alike in the art of organic synthesis since its introduction in 1996. In this highly welcomed new volume, K. C. Nicolaou and Scott A. Snyder discuss in detail the most impressive accomplishments in natural product total synthesis during the 1990s and the first years of the 21st century. While all of the features that made the first volume of Classics so popular and unique as a teaching tool have been maintained, in this new treatise the authors seek to present the latest techniques and advances in organic synthesis as they beautifully describe the works of some of the most renowned synthetic organic chemists of our time. · domino reactions, cascade sequences, biomimetic strategies, and asymmetric catalysis are systematically developed through the chosen synthesis · cutting edge synthetic technologies are discussed in terms of mechanism and scope · new reactions, such as olefin metathesis, are presented in mini-review style · abundant references are given for further reading Graduate students, educators, and researchers in the fields of synthetic and medicinal chemistry will wish to have a copy of this book in their collection as an indispensable companion that both augments and supplements the original Classics in Total Synthesis. From reviews of "Classics in Total Synthesis": "... a volume, (..) which any chemist with an interest in synthetic organic chemistry will wish to acquire." JACS "...this superb book (..) will be an essential purchase for many organic chemists." Nature
"The second edition of this classic text book has been completely revised, updated, and extended to include chapters on biomimetic amination reactions, Wacker oxidation, and useful domino reactions. The first-class author team with long-standing experience in practical courses on organic chemistry covers a multitude of preparative procedures of reaction types and compound classes indispensable in modern organic synthesis. Throughout, the experiments are accompanied by the theoretical and mechanistic fundamentals, while the clearly structured sub-chapters provide concise background information, retrosynthetic analysis, information on isolation and purification, analytical data as well as current literature citations. Finally, in each case the synthesis is labeled with one of three levels of difficulty. An indispensable manual for students and lecturers in chemistry, organic chemists, as well as lab technicians and chemists in the pharmaceutical and agrochemical industries."--P.  of cover.