Antifungal compound process
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
1. A process to prepare a compound of formula IX or IXa,
or a mixture thereof, the process comprising:
(i) combining compound 1 or 1a,
or a mixture thereof, a sulfonic acid
and a crystallization solvent or crystallization solvent mixture;
(ii) diluting the mixture from step (i) with a crystallization co-solvent or crystallization co-solvent mixture; and
(iii) isolating a compound of formula IX or IXa,
or a mixture thereof;
wherein each Z is independently aryl, substituted aryl, alkyl, or substituted alkyl.
2. The process of claim 1 , wherein Z is phenyl, p-tolyl, methyl, or ethyl.
3. The process of claim 1 , wherein the crystallization solvent or crystallization solvent mixture is ethyl acetate, isopropyl acetate, ethanol, methanol, or acetonitrile, or combinations thereof.
4. The process of claim 1 , wherein the crystallization co-solvent or crystallization co-solvent mixture is pentane, methyl tert-butylether, hexane, heptane, or toluene, or combinations thereof.