Enantiopure drug synthesis: From methyldopa to imipenem to efavirenz

An historical retrospective is presented relative to the development of practical processes for the syntheses of three major drugs: methyldopa, imipenem, and efavirenz. Each highlights a major method for asymmetric synthesis. This work was initially presented as a lecture at the BLOCKBUSTER CHIRALITY section of the CHIRALITY 2004 meeting in New York City, and this paper is simply a written account of that presentation. The original literature that details the chemistry discussed herein is noted in the reference section. (c) 2005 Wiley-Liss, Inc.