Palladium-catalyzed cross-coupling of unreactive C(sp3)–H bonds with azole C(sp2)–H bonds by using bromide as a traceless directing group

Abstract

A palladium-catalyzed intermolecular cross-coupling of unreactive C(sp³)–H bonds and azole C(sp²)–H bonds with bromide as a traceless directing group is described. The judicious selection of the bulky and electron-rich phosphine ligand is the key for the success of this cascade process. The protocol features a broad substrate scope, excellent regioselectivity, and good functional group tolerance.