Enantiomeric separation of (RS)1-(4-chlorophenyl)-2-chloroethanol by lipase catalyzed hydrolysis of its acetate

摘要

Process for the preparation of one or both enantiomers of 1-(4- chlorophenyl)-2-chloroethanol, which comprises an enantioselective enzymatic hydrolysis of (.+-.)-&agr;-(4-chlorophenyl)chloroethyl acetate by means of an enzyme which is horse liver acetone powder, lipase PS from Pseudomonas fluorescens, lipase AK from Pseudomonas or the lipase from Candida antarctica, to give a mixture of unhydrolysed R-(-)-&agr;- (4- chlorophenyl)chloroethyl acetate and S-(+)-1-(4-chlorophenyl)-2- chloroethanol, and optional separation of R-(-)-&agr;-(4-chlorophenyl) chloroethyl acetate and optional hydrolysis of it to give R-(-)-1-(4- chlorophenyl)-2-chloroethanol and use of the enantiomers of 1-(4- chlorophenyl)-2-chlorethanol for the preparation of the enantiomers of eliprodil and of their salts.