Amidation and Intramolecular Aza‐Michael Reaction: One‐Pot Synthetic Strategy of Isoindolinones

Herein, we report one‐pot Cu(I) catalyzed open flask synthetic strategy of 3‐substituted N ‐pyridinyl isoindolinones from alkyl ( E )‐3‐(2‐formylphenyl)acrylate by oxidative amidation and intramolecular aza‐Michael reaction using cheap air stable Cu(I) single catalyst. We have also established a synthetic route of N ‐aryl substituted isoindolinones with acid‐amine coupling reaction of ( E )‐2‐(3‐alkoxy‐3‐oxoprop‐1‐en‐1‐yl)benzoic acid followed by aza‐Michael reactions. Unexpected synthetic route of N ‐(1H‐inden‐1‐yl)pyridin‐2‐amine derivatives have been documented from the same precursors using Cu(I) catalyst.