The Process Development of Ravuconazole: An Efficient Multikilogram Scale Preparation of an Antifungal Agent1

摘要

The development of a safe, robust process for the preparation of ravuconazole (1), an antifungal agent, is described. The discovery and development of procedures enabling the efficient synthesis of multikilogram quantities of 1 and the process demonstration through plant scale preparations are presented. A controlled means to prepare a Grignard reagent and utilization of Fourier Trans-form Infrared spectroscopy (FTIR) monitoring to safely conduct the reaction is featured.