Synthetic Methods in Drug Discovery

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. This two-volume set of books provides both academic and industrial perspectives on 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. Moreover, key opportunities in expanding chemical space are presented, including the increasingly important syntheses that introduce three-dimensional molecular shape. Volume 1 focusses on transition metal mediated methods used in industry and volume 2 covers further valuable methods, such as fluorination, C-N bond formation and asymmetric reactions. Edited and authored by leading scientists from both academia and industry, this set of books will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.

Suzuki-Miyaura Coupling; Negishi Coupling; Hiyama Coupling; Sonogashira Coupling; Heck Coupling; Palladium- and Copper-Catalysed C-N Cross-Coupling in Drug Discovery; Chan-Lam Coupling Reaction; C-H Activation Approaches to Molecules; Palladium-Catalyzed Decarboxylative Couplings; New Frontiers with Transition Metals; Lithium, Magnesium, and Copper: Contemporary Applications of Organometallic Chemistry in the Pharmaceutical Industry; C-N Bond Formation via Hydrogen Transfer; Synthesis of Sulfonamides; Asymmetric Methods and Their Use in the Pharmaceutical Industry; Fluorination Approaches; The Development of Csp3-Csp2 Coupling Methodology; Catalytic Amide Bond Forming Methods; Accessing Novel Molecular Motifs and Monomers