Utilizing dimethy succinate and benzoic aldehyde as starting materials, Mitiglinide was synthesized with a high optical purity (> 99%) in the overall yield 10.7% via a ten-step route including Stobbe condensation, hydrolyzation, catalytic hydrogenation and resolution. 以琥珀酸二甲酯和苯甲醛等为起始原料,经过Stobbe缩合、水解、催化氢化、拆分等十步反应,合成了具有较高光学纯度(>99%)的Mitiglinide,总收率为10.7%。