Facile and stereospecific synthesis of diverse β- N -glycosyl sulfonamide scaffolds via palladium catalysis.

Glycosylation is an important strategy to improve the druggability of lead compounds. Here, we present a palladium-catalysed stereospecific N -glycosylation of sulfonamides. This approach stands out with wide substrate scope, high functional group tolerance, and easy scalability, furnishing a broad spectrum of densely functionalized β- N -glycosyl sulfonamides with good efficiency and exceptional regio-/stereoselectivity. Diverse drug-like glycosulfonamido scaffolds have been constructed via a late-stage diversification strategy and various facile synthetic transformations of the products. Collectively, the established protocol provides a valuable tool for efficiently preparing glycosyl sulfonamides to facilitate drug discovery.