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.
Inhoudsopgave
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
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