| 摘要 |
PROBLEM TO BE SOLVED: To obtain an optically active propionic acid derivative useful for pharmaceuticals, etc., in high purity and yield, i.e., high selectivity and high asymmetric yield by subjecting a specific substituted arylpropenoic acid derivative to asymmetric reduction (asymmetric hydrogenation) reaction. SOLUTION: The objective optically active propionic acid derivative of preferably formula II or III is produced by the asymmetric reduction of a 2- hydroxymethyl-3-arylpropenoic acid of preferably formula I (R1 is H, a lower alkyl or the like; and R2 is H or a hydroxy-protecting group) in the presence of preferably an optically active BINAP-metal complex as an asymmetric reduction catalyst. The hydroxyl group of each derivative may be protected and the aryl group may have substituents. The carboxyl group of each derivative may take an amide or ester form. An optically active 2-acylthiomethyl-3- arylpropionic acid useful as a synthetic intermediate for an enkephalinase inhibitor, etc. can be produced by using the derivative of formula II or III. |
