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.
Grabowski
Edward J J
EJ
Merck Research Laboratories, Merck & Company Incorporated, Rahway, New Jersey, USA. edjjg@bellatlantic.net