Cu(II)-Catalyzed N‑Directed Distal C(sp3)–H Heteroarylation of Aliphatic N‑Fluorosulfonamides

A copper-catalyzed δ-regioselective C­(sp3)–H heteroarylation of N-fluorosulfonamides has been developed. A broad range of heteroarenes were well tolerated and reacted with various N-fluorosulfonamides to give the corresponding heteroarylated amides in good yields. Notably, all types (1°, 2°, and 3°) of δ-C­(sp3)–H bonds in the N-fluorosulfonamides could be regioselectively activated through the 1,5-HAT process. This protocol provides a practical strategy for the functionalization of heteroarenes and amides via forging a C­(sp3)–C­(sp2) bond.