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Chapter contribution from Ben Feringa, Nobel Laureate in Chemistry 2016.Atropisomerism and Axial Chirality provides a global survey of the chemistry of axially chiral compounds including biaryls, heterobiaryls, non-biaryl atropisomers, allenes and spyrocyclic derivatives. From the perspective of a synthetic organic chemist, this book provides a unique compilation of the available methodologies for their synthesis, with emphasis on the most efficient and modern strategies, a review of the huge amount of practical applications in the field of asymmetric catalysis, either as transition metal ligands or as organocatalysts, and an overview of their occurrence as bioactive compounds and natural products.The first of its kind, this book serves as a general introduction and a practical reference to advanced chemistry students and researchers, while also offering creative ideas for further developments in the field.
Axially Chiral Compounds Explore this comprehensive and current volume summarizing the characteristics, synthesis, and applications of axial chirality Appearing widely in natural products, biologically active molecules, asymmetric chemistry, and material science, axially chiral motifs constitute the core backbones of the majority of chiral ligands and organocatalysts in asymmetric catalysis. In a new work of particular relevance to synthetic chemists, Axially Chiral Compounds: Asymmetric Synthesis and Applications delivers a clearly structured and authoritative volume covering the classification, characteristics, synthesis, and applications of axial chirality. A must read for every synthetic chemist practicing today, the book follows the development history, research status, and applications of axial chirality. An introductory chapter familiarizes the reader with foundational material before the distinguished authors describe the different classes and the synthesis of axial chiral compounds used in asymmetric synthesis. The book concludes with a focus on the applications of chiral ligands, chiral catalysts, and materials. Readers will also benefit from the inclusion of: A thorough introduction to asymmetric synthesis, including biaryls atropisomers, heterobiaryls atropisomers, and non-biaryls atropisomers Explorations of chiral allene, spiro skeletons, and natural products Practical discussions of asymmetric transformation, chiral ligands, and chiral catalysts An examination of miscellaneous applications of axially chiral compounds Perfect for organic chemists, chemists working with or on organometallics, catalytic chemists, and materials scientists, Axially Chiral Compounds: Asymmetric Synthesis and Applications will also earn a place in the libraries of natural products chemists who seek a one-stop reference for compounds exhibiting axial chirality.
This book describes the processes that are involved in the development of new drugs. The authors discuss the history, role of natural products and concept of receptor interactions with regard to the initial stages of drug discovery. In a single, highly readable volume, it outlines the basics of pharmacological screening, drug target identification, and genetics involved in early drug discovery. The final chapters introduce readers to stem therapeutics, pharmacokinetics, pharmacovigilance, and toxicological testing. Given its scope, the book will enable research scholars, professionals and young scientists to understand the key fundamentals of drug discovery, including stereochemistry, pharmacokinetics, clinical trials, statistics and toxicology.
Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.
Chiral materials have been studied in the Department of Chemistry at the University of Virginia for applications in areas like asymmetric catalysis, enantioselective fluorescent sensing, and optical/electrical materials. Optically active 1,1′-binaphthyl molecules are used to build novel chiral polymers, dendrimers, macrocycles, and acyclic molecules. 1,1′-Binaphthyl molecules are chosen because of their remarkably stable chiral configuration as well as their high asymmetric inductions in many processes.In this book, both the fundamental knowledge about the 1,1′-binaphthyl molecules and the synthesis of the structurally diverse 1,1′-binaphthyl-based materials are described. The applications of these materials in various fields are also discussed. This book will serve as a reference for graduate students as well as other professionals working in the related fields./a
Catalytic asymmetric synthesis has been one of the most active research areas in chemistry (Nobel Prize in 2001). The development of efficient chiral catalysts plays a crucial role in asymmetric catalysis. Although many chiral ligands/catalysts have been developed in the past decades, the most efficient catalysts are derived from a few core structures, called "privileged chiral catalysts". This ultimate "must have" and long awaited reference for every chemist working in the field of asymmetric catalysis starts with the core structure of the catalysts, explaining why a certain ligand or catalyst is so successful. It describes in detail the history, the basic structural characteristics, and the applications of these "privileged catalysts". This novel presentation provides readers with a much deeper insight into the topic and makes it a must-have for organic chemists, catalytic chemists, chemists working with/on organometallics, chemists in industry, and libraries. From the contents: * BINAP * Bisphosphacycles - From DuPhos and BPE to a Diverse Set of Broadly Applied Ligands * Josiphos Ligands: From Discovery to Technical Applications * Chiral Spiro Ligands * Chiral Bisoxazoline Ligands * PHOX Ligands * Chiral Salen Complexes * BINOL * TADDOLate Ligands * Cinchona Alkaloids * Proline Derivatives
While working as a chromatographer in the pharmaceutical industry, it became apparent to the editor that there was a pressing need for a comprehensive reference text for analysts working on the resolution of enantiomers by liquid chromatography (LC). This need arises from the fact that, whereas previously it was very difficult to determine enantiomers by direct means, there is now a wide choice of direct LC methods. At the same time, regulatory authorities have been changing their attitudes towards the administration of pharmaceuticals as racemates, partly because it is now possible to study the individual enantiomers. Clearly this abundance of new information needs to be rationalized. More importantly, the chiral LC systems which are commercially available or readily accessible to the practising chromatographer needed to be reviewed and, to a much greater extent than in existing reviews or books, discussed in terms of their practical application. Accordingly this book is very much orientated towards the practical aspects of these commercially available and readily accessible chiral LC systems. To this end, it is written for practising chromatographers by a team of practising, experienced chromatographers who have spent many years tackling the problems presented by resolving enantiomers by LC. The practical aspects of common chiral LC systems cannot be fully understood if discussed in isolation.
Aimed at advanced undergraduate and graduate students and researchers working with natural products, Professors Sunil and Bani Talapatra provide a highly accessible compilation describing all aspects of plant natural products. Beginning with a general introduction to set the context, the authors then go on to carefully detail nomenclature, occurrence, isolation, detection, structure elucidation (by both degradation and spectroscopic techniques) stereochemistry, conformation, synthesis, biosynthesis, biological activity and commercial applications of the most important natural products of plant origin. Each chapter also includes detailed references (with titles) and a list of recommended books for additional study making this outstanding treatise a useful resource for teachers of chemistry and researchers working in universities, research institutes and industry.
This book aims to guide and inspire drug researchers as they enter the 21st century. Stereochemistry is an essential dimension in pharmacology and should be understood as such by all drug researchers whatever their background. When used as probes or medicines, stereoisomeric drugs offer invaluable insights or innovative therapeutic strategies. The book spans the subject from the molecular to the clinical. The first section on chemical aspects contains chapters on chemical synthesis, analysis, natural products, chiral stability (racemezation) and physical properties. The second section is on experimental pharmacology, with chapters on drug-receptor interactions, chiral recognition, ion channels, and molecular toxicology. The third section focuses on drug disposition, with chapters on absorption, distribution, protein binding, metabolism and elimination. The final section is dedicated to regulatory and clinical aspects.
A compilation of research on the versatile reagent of cholorosulfonyl isocyanate (CSI). The text is divided into two parts. The first part outlines the reactions of CSI with a wide variety of substrates. The second part outlines the applications of CSI in the preparation of useful products.