Gold-catalyzed post-Ugi alkyne hydroarylation for the synthesis of 2-quinolones

Abstract

A series of propargylamides containing an electron-rich benzene ring was prepared via a Ugi four-component condensation. These adducts underwent gold-catalyzed intramolecular alkyne hydroarylation to efficiently construct the 2-quinolone core with N‑branched substituents. The method demonstrated broad substrate scope, high yields (up to 97 %), and favorable environmental profile using fluorinated alcohols as solvents.