INTERMEDIATE IN SYNTHESIS OF ENANTHIOMER OF ERYPROGYL AND PREPARATION THEREOF

摘要

Prodn. of enantiomers of 1-(4-chlorophenyl)-2-chloroethanol (I) comprises:(a) hydrolysing racemic ( plus or minus )- alpha -(4-chlorophenyl)chloroethyl acetate (II) with a lipase prepn.;(b) sepg. the resulting S(+)-1-(4-chlorophenyl)-2-chloroethanol (Ia) from the unhydrolysed R(-)- alpha -(4-chlorophenyl)chloroethyl acetate (IIa), opt. after converting (Ia) to its succinate (Ib), and(c) hydrolysing (IIa) and opt. (Ib). The lipase prepn. is equine liver acetone extract powder, Pseudomonas fluorescens lipase PS, Pseudomonas lipase AK or Candida antarctica lipase. Also claimed are (Ia) and (IIa) prepd. as above.