Cascade reaction involving Diels–Alder cascade: modular synthesis of amino α-pyrones, indolines and anilines

The Diels–Alder reaction is a famous and useful method for the synthesis of six-membered carbocycles and heterocycles, and the investigation to extend its power draws tremendous interests. Herein, we develop a coupling reaction for the modular synthesis of amino α-pyrones as Diels–Alder reaction precursors, and also establish the Diels–Alder cascade for obtaining indolines and anilines. This protocol features readily available starting materials, broad substrate scope and valuable synthetic utility.