Practical Synthesis of Phosphinic Amides/Phosphoramidates through Catalytic Oxidative Coupling of Amines and P(O)−H Compounds

Abstract Herein, we report a highly efficient ZnI 2 ‐triggered oxidative cross‐coupling reaction of P(O)−H compounds and amines. This operationally simple protocol provides unprecedented generic access to phosphinic amides/phosphoramidate derivatives in good yields and short reaction time. Besides, the reaction proceeds under mild conditions, which avoids the use of hazardous reagents, and is applicable to scale‐up syntheses as well as late‐stage functionalization of drug molecules. The stereospecific coupling is also achieved from readily available optically enriched P(O)−H compounds.