Building on key reactions presented in Volume 1, Synthetic Methods in Drug Discovery Volume 2 covers a range of important reaction types including organometallic chemistry, fluorination approaches and asymmetric methods as well as new and exciting areas such as Csp2-Csp3 couplings, catalytic amide bond forming reactions, hydrogen borrowing chemistry and methods to access novel motifs and monomers. This book 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. 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.
Table of Content
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 Csp
3-Csp
2 Coupling Methodology; Catalytic Amide Bond Forming Methods; Accessing Novel Molecular Motifs and Monomers
About the author
David Blakemore has spent his entire career in the pharmaceutical industry. Following his post-docs in Cambridge and Paris, he joined Warner-Lambert as a Group Leader in the Discovery Chemistry group. In 2001, he joined Pfizer in Sandwich and is currently the Synthesis Lead for the World-Wide Medicinal Chemistry Group at Pfizer Neusentis. Part of David’s role is in liaising with academics to highlight key areas of chemistry that could be of real value to the pharmaceutical industry and to develop interactions in those areas.
Paul Doyle has spent his entire career at the interface of chemistry and biology in the service of drug discovery. After his first degree in chemistry at Oxford, Paul completed his D.Phil. at the University of Sussex studying bio-organic synthetic chemistry. He spent a 15-year early career in a wide variety of therapeutic discovery programmes at the Wellcome Foundation before establishing one of the first UK discovery CROs, Biofocus. In 2008, Paul joined Peakdale as CEO.
Yvette Fobian has spent the majority of her career in the pharmaceutical industry. After completing her Ph D and spending a year in Monsanto’s Corporate Research, she joined the Medicinal Chemistry Group in Searle/Monsanto in 1997 and ultimately Pfizer in 2003 following a series of mergers and acquisitions. In her most current role, Yvette is in an excellent position to see first-hand the needs and impact of synthetic enablement for both small and large scale delivery within the discovery team.
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