Photoinduced Sulfur Hexafluoride-Promoted Site-Selective Phosphonylation of Amino Acids and Peptide Derivatives

α-Aminophosphonates are crucial molecular scaffolds in drug development due to their diverse biological activities. However, existing synthetic methods are often limited by a narrow substrate scope, harsh reaction conditions, or reliance on transition metal catalysts and strong oxidants, restricting their applicability. This work reports a photoinduced strategy for the site-selective phosphonylation of amino acids and peptide derivatives to synthesize α-aminophosphonates. The method utilizes sulfur hexafluoride (SF₆) as an electron acceptor and achieves its degradation during the reaction, enabling the effective utilization of greenhouse gas SF₆.