Direct Amidation of 2′-Aminoacetophenones Using I₂‑TBHP: A Unimolecular Domino Approach toward Isatin and Iodoisatin

Abstract

Synthesis of isatin and iodoisatin from 2′-aminoacetophenone was achieved via oxidative amido cyclization of the sp³ C–H bond using I₂–TBHP as the catalytic system. The reaction proceeds through sequential iodination, Kornblum oxidation, and amidation in one pot. This method is simple, atom economic, and works under metal- and base-free conditions