Preparation of (2,3-Dihydrobenzofuran-3-yl)acetic Acid via Rh-Catalyzed Asymmetric Hydrogenation

作者:Yamashita Masayuki*; Negoro Nobuyuki; Yasuma Tsuneo; Yamano Toru
来源:Bulletin of the Chemical Society of Japan, 2014, 87(4): 539-543.
DOI:10.1246/bcsj.20130324

摘要

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.

  • 出版日期2014-4-15