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.

Automated summary

A novel and cost-effective nickel-catalyzed ortho-C-Ar-H glycosylation reaction with high regioselectivity and excellent alpha-selectivity is described in this study. The method shows great functional group compatibility with various glycosides, demonstrating its synthetic potential. Mechanistic studies suggest that C-H activation could be the rate-determining step.