O'Brien M K, Vanasse B
Aventis Pharmaceuticals, Route 202-206, PO Box 6800, Bridgewater, NJ 08807, USA.
Curr Opin Drug Discov Devel. 2000 Nov;3(6):793-806.
More than 50% of the 500 top selling drugs in the world today are single enantiomers. To address the production of enantiomerically pure drug candidates, several tools (chiral pool, asymmetric catalysis, chiral reagents, chiral auxiliaries, resolution and biotransformation) are becoming increasingly available to the process chemist for development and large-scale manufacturing. This article will document salient examples from the post-1998 literature that, in the opinion of the authors, best exemplify the utilization of these tools by process chemistry groups throughout the pharmaceutical industry.
当今世界最畅销的500种药物中，超过50%是单一对映体。为了满足对映体纯的候选药物的生产需求，过程化学家在药物开发和大规模生产中可利用的工具（手性源、不对称催化、手性试剂、手性助剂、拆分和生物转化）越来越多。本文将记录1998年之后文献中的突出实例，作者认为这些实例最能体现制药行业各过程化学团队对这些工具的运用。
