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

Org Lett. 2022 Feb 4;24(4):1055-1059. doi: 10.1021/acs.orglett.1c04280. Epub 2022 Jan 26.

Abstract

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.