Details

Autor(en) / Beteiligte

• Genovino, Julien
• Sames, Dalibor
• Hamann, Lawrence G.
• Touré, B. Barry

Titel

Accessing Drug Metabolites via Transition-Metal Catalyzed C−H Oxidation: The Liver as Synthetic Inspiration

Ist Teil von

• Angewandte Chemie (International ed.), 2016-11, Vol.55 (46), p.14218-14238

Auflage

International ed. in English

Ort / Verlag

Germany: Blackwell Publishing Ltd

Erscheinungsjahr

2016

Quelle

MEDLINE

Beschreibungen/Notizen

• Can classical and modern chemical C−H oxidation reactions complement biotransformation in the synthesis of drug metabolites? We have surveyed the literature in an effort to try to answer this important question of major practical significance in the pharmaceutical industry. Drug metabolites are required throughout all phases of the drug discovery and development process; however, their synthesis is still an unsolved problem. This Review, not intended to be comprehensive or historical, highlights relevant applications of chemical C−H oxidation reactions, electrochemistry and microfluidic technologies to drug templates in order to access drug metabolites, and also highlights promising reactions to this end. Where possible or appropriate, the contrast with biotransformation is drawn. In doing so, we have tried to identify gaps where they exist in the hope to spur further activity in this very important research area. Organic synthesis: This Review addresses an important question of great practical significance in the pharmaceutical industry: can classical and modern chemical C−H oxidation reactions complement biotransformation in the synthesis of drug metabolites? Drug metabolites are required throughout all phases of the drug discovery and development process; however, their synthesis is still an unsolved problem.