Synthetic Communications p. 3373 - 3379 (2019)
Update date:2022-08-29
Topics:
Hu, Lin
Zou, Ping
Wei, Wanguo
Yuan, Xi-Meng
Qiu, Xiao-Long
Gou, Shao-Hua
A facile and green synthetic route was developed for the preparation of dapagliflozin (1), 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 (1) more efficiently. The synthetic route featured the usage of commercial available and easily handling reagents with shorter reaction steps and less waste disposal.
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(2019)