Efficient One-Step Synthesis of a Key Intermediate for the Synthesis of Azole Antifungals Using the Mitsunobu Protocol.

Abstract A simple and single‐step process for coupling (2R,1S)‐1‐[2‐(2,4‐difluorophenyl)‐2‐oxiranyl]ethanol and various 1,2,4‐triazolones utilizing the Mitsunobu protocol is described. The product so formed is a key intermediate in the synthesis of azole antifungals with potent and broad‐spectrum activity against yeast and filamentous fungi.