Copper-Catalyzed N-Arylation of Sulfamates and Sulfamides

Abstract Sulfamates and sulfamides are privileged motifs in medicinal chemistry, yet direct methods for assembling their N-(hetero)aryl derivatives remain limited. We report a unified Cu-catalyzed protocol for the N-arylation of sulfamates and sulfamides with aryl- and heteroaryl bromides that is operationally simple, cost-effective, scalable, and broadly applicable to pharmacologically relevant substrates. Copper-catalyzed N-arylations can also be combined with HFIPS sulfamoylations to access N-aryl sulfamates and sulfamides in telescoped or one-pot sequences from alcohol and amine precursors.