2-Benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid → Mitiglinide

Participants

Reaction Steps

The preparation was carried out in the same manner as in Example 1, except that 1.94 mg of rhodium-1,5-cyclooctadiene-tetrafluoroboric acid complex hydrate (S/C=10000) was used instead of 1.18 mg of rhodium-1,5-cyclooctadiene-chloride complex of Example 1. After the reaction, the residual ratio of 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid was 2.21%, and the optical purity of mitiglinide thus obtained was 95.9% e.e.

Provenance & Evidence