Highly Regioselective And Stereoselective Synthesis Of C-Aryl Glycosides Via Nickel-Catalyzed Ortho-C-H Glycosylation Of 8-Aminoquinoline Benzamides

C-Aryl glycosides are of high value as drug candidates. Here a novel and cost-effective nickel catalyzed ortho-C-Ar-H glycosylation reaction with high regioselectivity and excellent alpha-selectivity is described. This method shows great functional group compatibility with various glycosides, showing its synthetic potential. Mechanistic studies indicate that C-H activation could be the rate-determining step.