Gold-Catalyzed Cascade Reaction of β-(2-Aminophenyl)-α,β-ynones with Ynamides: A Sequential Route to Polysubstituted 2-Aminoquinolines.

A novel, efficient, and mild synthetic route for the preparation of 2-aminoquinolines via a gold-catalyzed cascade reaction of β-(2-aminophenyl)-α,β-ynones with ynamides has been developed. This process tolerates a wide range of functionalities such as halogen, alkyl, aryl, and heteroaryl groups, leading to original heterocycles in fair to very good yields.