Direct dehydrative cross-coupling of tautomerizable heterocycles with alkynes via Pd/Cu-catalyzed phosphonium coupling

The first chemoselective direct dehydrative cross-coupling of tautomerizable heterocycles with alkynes has been achieved via C–H/C–OH bond activations with direct C(sp2)–C(sp) bond formation, which is in line with ideal synthesis using readily available materials.