Efficient and Scalable Synthesis of Glucokinase Activator with a Chiral Thiophenyl-Pyrrolidine Scaffold

Efficient and Scalable Synthesis of Glucokinase Activator with a Chiral Thiophenyl-Pyrrolidine Scaffold

Hiroki Fujieda* , Koji Maeda, and Noriyasu Kato

Sanwa Kagaku Kenkyusho Co., Ltd., 35 Higashisotobori-cho, Higashi-ku, Nagoya-shi, Aichi 461-8631, Japan

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.8b00354

Publication Date (Web): December 11, 2018

Copyright © 2018 American Chemical Society

*E-mail: h_fujieda@skk-net.com.

Cite this:Org. Process Res. Dev.  XXXX, XXX, XXX-XXX

Abstract

Abstract Image

Herein we describe the practical synthesis of a potent glucokinase activator (1) that has a chiral thiophenyl-pyrrolidine scaffold. The key to the successful synthesis was the application of a telescoped chiral-pool synthesis from a comm