Fluorosulfonamide-Directed Heteroarylation of Aliphatic C(sp3)-H Bonds

J Org Chem. 2023 Apr 7;88(7):4757-4760. doi: 10.1021/acs.joc.2c02461. Epub 2023 Mar 13.

Abstract

Herein, we describe a formal dehydrogenative cross coupling of heterocycles with unactivated aliphatic amines. The resulting transformation enables the direct alkylation of common heterocycles by merging N-F-directed 1,5-HAT with Minisci chemistry, leading to predictable site selectivity. The reaction provides a direct route for the transformation of simple alkyl amines to value-added products under mild reaction conditions, making this an attractive option for C(sp3)-H heteroarylation.