PRODUCTION OF OPTICALLY ACTIVE 2-BENZYLSUCCINIC ACID

摘要

PROBLEM TO BE SOLVED: To produce optically active 2-benzylsuccinic acid selectively and at a high yield by making (SR)-2-benzylsuccinic acid react with a specific optically active amine derivative as an agent for optical resolution. SOLUTION: This optically active (s)- or (R)-2-benzylsuccinic acid is produced (A) by making recemic 2-benzylsuccinic acid of formula I (asterisked C is an asymmetric carbon) react preferably with 0.5-2.5 equivalent of an optically active amine derivative [e.g. a compound of formula II (R<1> and R<2> are H, an lower alkyl; R<3> is a lower alkyl; R<4> is phenyl or an aralkyl) (e.g. (+) or (-)-1- phenylethlyamine)] at 25-90 deg.C to form a diastereometric salt, and (B) by subjecting the above-mentioned diastereometric salt to acid or alkali treatment at 5-30 deg.C.