PROCESS FOR PREPARING INTERMEDIATES FOR THE SYNTHESIS OF ANTIFUNGAL AGENT

摘要

PROBLEM TO BE SOLVED: To provide a process for producing a large excess of a crystalline chiral hydroxy ester.

SOLUTION: There is provided a process for preparing the crystalline chiral hydroxy esters of Formula 1.0 by the stereoselective acylation of a diol of a Formula 2.0 with isobutyric anhydride. The process comprises reacting a diol of Formula 2.0 with isobutyric anhydride and a lipase enzyme in a suitable organic solvent (e.g., acetonitrile) at a low temperature. A sufficient amount of enzyme and isobutyric anhydride is used to allow the reaction to proceed at a reasonable rate to the formation of the chiral hydroxy ester while keeping the formation of diesters to a minumum.

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