Preparation of (2,3-dihydrobenzofuran-3-yl)acetic acid via Rh-catalyzed asymmetric hydrogenation

Article abstract of DOI:10.1246/bcsj.20130324

A preparation via Rh-catalyzed asymmetric hydrogenation has been developed for (2,3-dihydrobenzofuran-3-yl)-acetic acid derivatives, a key intermediate in the synthesis of the active pharmaceutical ingredient for GPR40 agonist, fasiglifam. Use of a cationic rhodium-Et-FerroTANE complex yielded the desired product in high enantiomeric excess (91%) and quantitative yield, and was thus recommended for further process development.