Sustainable N -Formylation of Amines through Catalyst-Free Aerobic C–C Bond Cleavage at Room Temperature

Abstract

Although numerous studies have been conducted on the N-formylation of amines, few approaches combine mild operating conditions with low process mass intensity (PMI). We report a sustainable N-formylation protocol that proceeds through catalyst-free aerobic C─C bond cleavage. Readily available aldehydes with suitable structural features serve as effective formyl sources, enabling the N-formylation to proceed at room temperature and exhibiting broad functional group tolerance. In addition, the reaction requires no additives and can be conducted at a high concentration, resulting in favorable PMI. Broad solvent compatibility and streamlined reaction and product isolation further reduce material and solvent consumption, underscoring the practical advantages of the proposed sustainable N-formylation protocol.