Regulating the Non‐Noble Metal Catalyst Cu@UiO‐67‐bpy Facilitates the Visible Light‐Induced Regioselective Acetylation of Terminal Alkynes With Arylamines

ABSTRACT The development of heterogeneous catalysts for the efficient construction of acetamide frameworks under mild conditions is of great significance for green pharmaceutical synthesis. An efficient and reusable heterogeneous Cu@UiO‐67‐bpy catalyst is synthesized by a standard solvothermal method and post‐synthetic metalation (PSM) procedures. This catalyst is fully characterized by using scanning electron microscopy (SEM), transmission electron microscopy (TEM), X‐ray diffraction (XRD), Fourier transform infrared spectra (FT‐IR), X‐ray photoelectron spectroscopy (XPS), and the Brunauer–Emmett–Teller (BET) method. The catalyst efficiently promotes the regioselective C–N coupling of arylamines with terminal alkynes, affording bioactive acetamide‐based pharmaceutical intermediates in excellent yields under visible light with O 2 as the oxidant. Owing to the heterotic nature of the catalyst, it can be easily separated by simple filtration from the reaction mixture and reused five times without obvious activity loss.