Palladium-Catalyzed Arylation of Amino-Carbasugar Enables the Discovery of a Potent and Selective Carbocyclic SGLT2 Inhibitor

September 28, 2016

Abstract: Selective inhibition of the transporter protein sodium‐glucose cotransporter 2 (SGLT2) has emerged as a promising way to control blood glucose level in diabetes patients. Reported herein is a short and convergent synthetic route towards some small‐molecule SGLT2 inhibitors by a chemo‐ and diastereospecific palladium‐catalyzed arylation reaction. This synthetic strategy enabled the discovery of two highly selective and potent SGLT2 inhibitors, thereby paving the way towards the development of carbasugar SGLT2 inhibitors as potential antidiabetic/antitumor agents.


Angew. Chem. Int. Ed., 2016, 55, 13818−13821.



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