Production of optically active 2-(2,5-dioxo-1-imidazolidinyl)acetic acid derivatives, useful as pharmaceutical intermediates, comprises stereoselective enzymatic hydrolysis of a mixture of enantiomers with an esterase

摘要

Production of optically active 2-(2,5-dioxo-1-imidazolidinyl)acetic acid derivatives (I), comprises: (1) enzymatic hydrolysis of a mixture of enantiomers with an esterase: and (2) separation of the converted and unconverted compounds from each other. Production of optically active 2-(2,5-dioxo-1-imidazolidinyl)acetic acid derivatives of formula (I), comprises: (1) enzymatic hydrolysis of a mixture of enantiomers of formula (I;R3=R3') with an esterase: and (2) separation of the converted and unconverted compounds from each other. R1 = H, F, or 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl or 3-4C cycloalkyl (optionally substituted by 1-3 of F, Cl, Br and Me); R1+R1 = (CH2)4 or (CH2)5; R2 = F, Cl, Br, NO2, CN, OH, OMe, acetylamino, t-butoxycarbonylamino, benzyloxycarbonylamino, SMe, t-butylthio, 1-10C alkyl, aryl, aryl(1-10C)alkyl, heteroaryl, heteroaryl(1-10C)alkyl, 2-10C alkenyl, 2-10C alkynyl, 3-7C cycloalkyl or (3-7C)cycloalkyl(1-10C)alkyl optionally substituted with 1-3 of halo, CF3, Me, NO2, CN, acetylamino, 9-fluorenylmethoxycarbonyl, t-butoxycarbonylamino, benzyloxycarbonylamino, SH, SMe, t-butylthio, OH, OMe, OEt or COOR4; R3 = H or R3'; R3' = 1-10C alkyl, aryl(1-10C)alkyl, 2-10C alkenyl, 2-10C alkynyl, 3-7C cycloalkyl or (3-7C)cycloalkyl(1-10C)alkyl optionally substituted with 1-3 of halo, CF3, Me, NO2, CN, acetylamino, t-butoxycarbonylamino, benzyloxycarbonylamino, SH, SMe, t-butylthio, OH, OMe, OEt and COOR5; and R4, R5 = H, 1-4C alkyl, 2-4C alkenyl or aryl(1-10C)alkyl.