An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

Beilstein J Org Chem. 2011:7:442-95. doi: 10.3762/bjoc.7.57. Epub 2011 Apr 18.

Abstract

This review presents a comprehensive overview on selected synthetic routes towards commercial drug compounds as published in both journal and patent literature. Owing to the vast number of potential structures, we have concentrated only on those drugs containing five-membered heterocycles and focused principally on the assembly of the heterocyclic core. In order to target the most representative chemical entities the examples discussed have been selected from the top 200 best selling drugs of recent years.

Keywords: five-membered rings; heterocycles; medicinal chemistry; pharmaceuticals; synthesis.