PROCESS FOR THE MANUFACTURE OF ENANTIOMERICALLY PURE ANTIFUNGAL AZOLES AS RAVUCONAZOLE AND ISAVUCONAZOLE

摘要

Methods for the preparation of enantiomerically pure azole compounds of formula I are disclosed. In particular resolution of a racemic mixture of a compound of formula I is performed by addition of a chiral acid, collection of the desired diastereomer followed by conversion of the salt into an enantiomerically pure form of the compound of formula I by treatment with a base or ion-exchange resin. Also disclosed is a method of resolving a racemic precursor of formula I followed by reaction of the enantiomerically pure precursor to form a compound of formula I.