Signposts to Chiral Drugs: Organic Synthesis in Action

Highlighting 15 selected chiral structures, which represent candidate or marketed drugs, and their chemical syntheses, the authors acquaint the reader with the fascinating achievements of synthetic and medicinal chemistry. The book starts with an introduction treating the discovery and development of a new drug entity. Each of the 15 subsequent chapters presents one of the target structures and begins with a description of its biological profile as well as any known molecular mechanisms of action, underlining the importance of its structural and stereochemical features. This section is followed by detailed discussions of synthetic approaches to the chiral target structure, highlighting creative ideas, the scaling-up of laboratory methods and their replacement by efficient modern technologies for large-scale production. Nearly 60 synthetic reactions, most of them stereoselective, catalytic or biocatalytic, as well as chiral separating methodologies are included in the book. Vitomir Sunjic and Michael J. Parnham provide an invaluable source of information for scientists in academia and the pharmaceutical industry who are actively engaged in the interdisciplinary development of new drugs, as well as for advanced students in chemistry and related fields.

Table of Contents:
Organic synthesis in drug discovery and development.- Aliskiren fumarate.- (R)-K-13675.- Sitagliptin phosphate monohydrate.- Biaryl unit in valsartan and vancomycin.- 3-Amino-1,4-benzodiazepines.- Sertraline.- 1,2-Dihydroquinolines.- (-)-Menthol.- Fexofenadine hydrochloride.- Montelukast sodium.- Thiolactone peptides as antibacterial peptidomimetics.- Efavirenz.- Paclitaxel.- Neoglycoconjugate.- 12-Aza  

Review :
From the reviews: “In this timely book, Šunjić and Parnham provide an exciting selection of major achievements in drug development and unfold 15 intriguing success stories of aliskiren, vancomycin, paclitaxel, menthol, efavirenz, and others from the perspective of a medicinal chemist. … This book will be most appealing to undergraduate and graduate students with an interest in synthesis and stereochemistry … . it should be considered an instructive teaching supplement that underscores the general significance and impact of creative synthetic chemistry and stimulates further discussion in the classroom.” (Christian Wolf, Journal of the American Chemical Society, September, 2011) “The subject of the book are chiral drugs. … Each chapter can be read separately and consists of an abstract, introduction, the main part with the synthetic approach to a certain drug, conclusion and references. … References are relevant and up-to date. A long list of abbreviations and acronyms is provided at the beginning … . The book will be very useful to synthetic organic and medicinal chemists in innovative pharmaceutical companies and to scientists and ambitious students of chemistry and pharmacy.” (Branka Zorc, Acta Pharmaceutica, Vol. 61, 2011) “This … volume will be of interest to those working in synthetic organic chemistry, particularly in the medicinal chemistry area, and having as their aim the discovery of new drug entities for the pharmaceutical industries. … there is also a useful summary of synthetic methods and concepts that are developed in the individual chapters, together with a useful index. The standard of presentation is very high, with many clearly presented reaction schemes, and each chapter has a comprehensive list of references to the specific area.” (D. W. Allen, Inflammopharmacology, Vol. 19, 2011)