PRODUCTION OF STEREOISOMETRICALLY PURE PHYNYLGLYCIDE ACID ESTER AND PRODUCTION OF (2S, 3S)-2-(4'-METHOXYPHENYL)-3-ACETOXY-5-(2-(DIMETHY LAMINO)ETHYL)-2, 3-DIHYDRO-1, 5-BENZODIAZEPIN- 4(5H)-ON

摘要

PURPOSE: To produce a pure phenylglycidic acid ester by enzymatically hydrolyzing an isomer mixture of esters of trans-phenylglycidic acid derivatives with a lipase, etc., and isolating an unhydrolyzed ester. ;CONSTITUTION: A mixture of isomers of esters of trans-phenylglycidic acid derivatives is enzymatically hydrolyzed with a proper lipase, a peptidase or a proteolytic bacterial enzyme. Then, unhydrolyzed (2R, 3S) ester is isolated from the reaction mixture to provide the objective stereoisomerically pure phenylglycidic acid represented by formula I (R₁ is an alkyl group; R₂ is hydrogen atom or an alkyl group). The enzymatic hydrolysis of the phenylglycidic acid esters is preferably carried out in a mixture of water with an organic solvent at ambient temperature up to about 60°C.;COPYRIGHT: (C)1990,JPO