Palladium-catalyzed cross-coupling of unreactive C(sp 3 )-H bonds with azole C(sp 2 )-H bonds by using bromide as a traceless directing group.

A palladium-catalyzed intermolecular cross-coupling of unreactive C(sp 3 )-H bonds and azole C(sp 2 )-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.