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. [ABSTRACT FROM AUTHOR]