Highly Efficient and Versatile Pd-Catalyzed Direct Alkynylation of Both Azoles and Azolines

Abstract

A highly efficient and versatile Pd-catalyzed direct alkynylation reaction of heterocycles with 1-bromoalkynes was developed. The substrate scope of the reaction was very broad to include not only azoles but also azolines for the first time, thus offering an important advance in the direct functionalization of heterocycles.