A Robust Copper-Catalyzed Cross-Coupling of Glycosyl Thiosulfonate and Boronic Acids Enables the Construction of Thioglycosides.

An efficient and stereoretentive copper-catalyzed cross-coupling of glycosyl thiosulfonate and boronic acid for the construction of thioglycosides is described. The good functional group compatibility of this method allows the preparation of many bioactive aryl/alkenyl thioglycosides, including the hSGLT1 inhibitor.