Chiral synthesis of tertiary alcohols with a hydrolase

摘要

PCT No. PCT/GB94/00793 Sec. 371 Date Dec. 11, 1995 Sec. 102(e) Date Dec. 11, 1995 PCT Filed Apr. 15, 1994 PCT Pub. No. WO94/24305 PCT Pub. Date Oct. 27, 1994Method of preparing an optically active compound of formula, wherein R and R1 are independently alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl, cycloalkyl, aryl, aralkyl, a heterocyclic group or a C1-C4 alkyl-heterocycle, each being optionally substituted, procided that R and R1 are not identical and * is an optically active chiral center, from the corresponding racemic ester or diol by treating with a hydrolase enzyme. In particular, racemic 2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-1,2 diol, an intermediate in fluconazole synthesis, is resolved using porcine pancreatic lipase or lipase from Chromobacterium viscosum.