Intermediates in the synthesis of the enantiomers of...

C - Chemistry – Metallurgy – 12 – P

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C12P 41/00 (2006.01) C07C 31/36 (2006.01) C07C 33/46 (2006.01) C07C 69/63 (2006.01) C07D 211/18 (2006.01) C12P 7/22 (2006.01)

Patent

CA 2166013

Process for the preparation of one or both enantiomers of 1-(4-chlorophenyl)-2-chloroethanol, which comprises an enantioselective enzymatic hydrolysis of ()-.alpha.-(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-(-)-.alpha.-(4-chlorophenyl)chloroethyl acetate and S-(+)-1-(4-chlorophenyl)-2-chloroethanol, and optional separation of R-(-)-.alpha.-(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.

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