One-Pot Synthesis of Multisubstituted 2‑Aminoquinolines from Annulation of 1‑Aryl Tetrazoles with Internal Alkynes via Double C–H Activation and Denitrogenation

An efficient, one-pot synthesis of multisubstituted 2-aminoquinolines from 1-aryl tetrazoles and internal alkynes has been developed. The reaction involves cyclization of 1-aryl tetrazoles with internal alkynes via rhodium­(III)-catalyzed double C–H activation and copper­(II)-mediated denitrogenation.