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 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.