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This book focuses on the drug discovery and development applications of transition metal catalyzed processes, which can efficiently create preclinical and clinical drug candidates as well as marketed drugs. The authors pay particular attention to the challenges of transitioning academically-developed reactions into scalable industrial processes. Additionally, the book lays the groundwork for how continued development of transition metal catalyzed processes can deliver new drug candidates. This work provides a unique perspective on the applications of transition metal catalysis in drug discovery and development – it is a guide, a historical prospective, a practical compendium, and a source of future direction for the field.
This book focuses on the drug discovery and development applications of transition metal catalyzed processes, which can efficiently create preclinical and clinical drug candidates as well as marketed drugs. The authors pay particular attention to the challenges of transitioning academically-developed reactions into scalable industrial processes. Additionally, the book lays the groundwork for how continued development of transition metal catalyzed processes can deliver new drug candidates. This work provides a unique perspective on the applications of transition metal catalysis in drug discovery and development – it is a guide, a historical prospective, a practical compendium, and a source of future direction for the field.
Transition metals open up new opportunities for synthesis, because their means of bonding and their reaction mechanisms differ from those of the elements of the s and p blocks. In the last two decades the subject has mushroomed - established reactions are seeing both technical improvements and increasing numbers of applications, and new reactions are being developed. The practicality of the subject is demonstrated by the large number of publications coming from the process development laboratories of pharmaceutical companies, and its importance is underlined by the fact that three Nobel prizes have been awarded for discoveries in this field in the 21st Century already. Organic Synthesis Using Transition Metals, 2nd Edition considers the ways in which transition metals, as catalysts and reagents, can be used in organic synthesis, both for pharmaceutical compounds and for natural products. It concentrates on the bond-forming reactions that set transition metal chemistry apart from "classical" organic chemistry. Each chapter is extensively referenced and provides a convenient point of entry to the research literature. Topics covered include: introduction to transition metals in organic synthesis coupling reactions C-H activation carbonylative coupling reactions alkene and alkyne insertion reactions electrophilic alkene and alkyne complexes reactions of alkyne complexes carbene complexes h3- or p-allyl -allyl complexes diene, dienyl and arene complexes cycloaddition and cycloisomerisation reactions For this second edition the text has been extensively revised and expanded to reflect the significant improvements and advances in the field since the first edition, as well as the large number of new transition metal-catalysed processes that have come to prominence in the last 10 years – for example the extraordinary progress in coupling reactions using “designer” ligands, catalysis using gold complexes, new opportunities arising from metathesis chemistry, and C-H activation – without neglecting the well established chemistry of metals such as palladium. Organic Synthesis Using Transition Metals, 2nd Edition will find a place on the bookshelves of advanced undergraduates and postgraduates working in organic synthesis, catalysis, medicinal chemistry and drug discovery. It is also useful for practising researchers who want to refresh and enhance their knowledge of the field.
Demonstrates the advantages of catalytic cascade reactions for synthesizing natural products and pharmaceuticals Riding the wave of green chemistry, catalytic cascade reactions have become one of the most active research areas in organic synthesis. During a cascade reaction, just one reaction solvent, one workup procedure, and one purification step are needed, thus significantly increasing synthetic efficiency. Featuring contributions from an international team of pioneers in the field, Catalytic Cascade Reactions demonstrates the versatility and application of these reactions for synthesizing valuable compounds. The book examines both organocatalysis and transition-metal catalysis reactions, bringing readers up to date with the latest discoveries and activities in all major areas of catalytic cascade reaction research. Catalytic Cascade Reactions begins with three chapters dedicated to organocatalytic cascade reactions, exploring amines, Brønsted acids, and the application of organocatalytic cascade reactions 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, and allenes Application of transition-metal catalyzed cascade reactions in natural product synthesis and drug discovery Engineering mono- and multifunctional nanocatalysts for cascade reactions Multiple-catalyst-promoted cascade reactions All chapters are thoroughly referenced, providing quick access to important original research findings and reviews so that readers can explore individual topics in greater depth. Drawing together and analyzing published findings scattered across the literature, this book provides a single source that encapsulates our current understanding of catalytic cascade processes. Moreover, it sets the stage for the development of new catalytic cascade reactions and their applications.
Homogeneous catalysis is an important strategy for the synthesis of high-valued chemicals. L. Brandsma has carefully selected and checked the experimental procedures illustrating the catalytic use of copper, nickel, and palladium compounds in organic synthesis. All procedures are on a preparative scale, make economic use of solvents and catalysts, avoid toxic substances and have high yields.
Im Laufe der vergangenen 35 Jahre wurden unzahlige Synthesewege entwickelt, bei denen Ubergangsmetallkomplexe entweder als Reagenzien oder als Katalysatoren fungieren. Dieses Buch bietet besonders denjenigen Synthesechemikern interessante und moderne Einblicke, die bisher noch nicht mit den vielfaltigen Moglichkeiten der Organometallchemie mit Ubergangsmetallen vertraut sind. Zu wichtigen ubergangsmetallkatalysierten Reaktionen werden Anwendungsbeispiele diskutiert. (01/00)
Organic reactions have wide spread applications in drug development, chemical biology, and materials science. However, traditional chemical techniques can be inefficient i.e., low yields and/or poor selectivity, for constructing structurally complex motifs and for selectively activating strong bonds. To address these problems, there has been an increasing focus on developing new organic reactions catalyzed by transition metals. This document describes my contributions to transition metal catalysis and includes the following works: 1) Catalytic activation of a single C-F bond in trifluoromethyl arenes for the synthesis of difluoromethyl arenes, 2) Mild copper-catalyzed fluorination of alkyl triflates using potassium fluoride, 3) Copper-catalyzed reduction of alkyl triflates and iodides: an efficient method for the deoxygenation of primary and secondary alcohols, 4) Synthesis of hindered anilines, and 5) Synthesis of tertiary alkyl amines from terminal alkenes: copper-catalyzed amination of alkyl boranes. For each work, I will describe its significance to organic synthesis, its discovery and development, and the investigation of its mechanism.
Transition metal catalysis belongs to the most important chemical research areas because a ubiquitous number of chemical reactions are catalyzed by transition metal compounds. Many efforts are being made by industry and academia to find new and more efficient catalysts for chemical processes. Transition metals play a prominent role in catalytic research because they have been proven to show an enormous diversity in lowering the activation barrier for chemical reactions. For many years, the search for new catalysts was carried out by trial and error, which was costly and time consuming. The understanding of the mechanism of the catalytic process is often not very advanced because it is difficult to study the elementary steps of the catalysis with experimental techniques. The development of modern quantum chemical methods for calculating possible intermediates and transition states was a breakthrough in gaining an understanding of the reaction pathways of transition metal catalyzed reactions. This volume, organized into eight chapters written by leading scientists in the field, illustrates the progress made during the last decade. The reader will obtain a deep insight into the present state of quantum chemical research in transition metal catalysis.
Author : David C. Blakemore Publisher : Royal Society of Chemistry Page : 474 pages File Size : 22,41 MB Release : 2016 Category : Medical ISBN : 1849738033
The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.