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

Synthesis of isatin and iodoisatin from 2'-aminoacetophenone was achieved via oxidative amido cyclization of the sp(3) 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.