Access to Functionalized Amines and Medium N-Heterocycles via Amine-Enabled Remote C–H Alkynylation

Abstract

By using weakly coordinating amines, we developed remote C−H alkynylation with precise control of reactivity and regioselectivity, enabling modification of complex drugs, natural products, and materials. The readily transformable alkyne-containing amine products would facilitate expedient delivery of molecular libraries of functionalized amines and medium N-heterocycles, which are previously elusive to access. Moreover, the introduced alkyne functionality could serve as a versatile handle to expand the diversity and synthetic application of this remote C−H functionalization.