Access to Functionalized\nAmines and Medium <i>N</i>‑Heterocycles via Amine-Enabled\nRemote C–H\nAlkynylation

By using weakly coordinating amines,\nwe developed remote\nC–H\nalkynylation with precise control of reactivity and regioselectivity,\nenabling modification of complex drugs, natural products, and materials.\nThe readily transformable alkyne-containing amine products would facilitate\nexpedient delivery of molecular libraries of functionalized amines\nand medium <i>N</i>-heterocycles, which are previously elusive\nto access. Moreover, the introduced alkyne functionality could serve\nas a versatile handle to expand the diversity and synthetic application\nof this remote C–H functionalization.