Dual Functionalization of α-Aminoamides via Photocatalytic Intramolecular Oxygen Migration to Cyanomethylureas

A green and efficient visible-light-driven strategy for direct cyanomethylurea synthesis from α-aminoamides and isothiocyanates via intramolecular oxygen migration is reported. This method merges cyanation and ureidation in a single step, leveraging the amide oxygen as a dual synthon to forge nitrile (C≡N) and urea (C═O) bonds. Operating under metal-free, ambient conditions (room temperature, air, visible light), the protocol accommodates diverse substrates without toxic reagents. Mechanistic studies implicate light-mediated desulfurization and oxygen atom transfer, offering a sustainable strategy for one-step dual functionalization of bioactive molecules.