Nickel-catalysed alkylation of C(sp3)–H bonds with alcohols: direct access to functionalised N-heteroaromatics

Abstract

The first base-metal catalysed coupling of primary alcohols with methyl-N-heteroaromatics is reported. The use of an earth abundant and nonprecious NiBr₂/L1 system enables access to a series of C(sp³)-alkylated N-heteroaromatics. Mechanistic studies have established the participation of a hydrogen-borrowing strategy for α-alkylation.