Wisdom Pharmaceutical Co., Ltd.

A facile and green synthetic route was developed for the preparation of dapagliflozin, a selective sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes.Key reaction steps include a direct Friedel-Crafts acylation and a synthesis of diaryl ketal moiety in one-pot manner without waste water generation.Furthermore, the reduction of the diaryl ketone and C-phenylglucoside were achieved in one-pot manner to generate dapagliflozin more efficiently.The synthetic route featured the usage of com. available and easily handling reagents with shorter reaction steps and less waste disposal.