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
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.
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.
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.
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.
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
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