Résumé
A novel Ru‐catalyzed asymmetric transfer hydrogenation (ATH) strategy has been developed for the efficient synthesis of valuable chiral α‐aminophosphonates from readily available α‐iminophosphonates. This method enables the conversion of both acyclic and cyclic substrates in high yields (up to 97%) and excellent enantioselectivities (up to >99:1), providing a practical entry to phosphorus‐containing chiral amines. Notably, this is the first reported application of ATH to α‐iminophosphonates, offering a robust and operationally convenient alternative to conventional asymmetric hydrogenation (AH) approaches. This study reports the first Ru‐catalyzed ATH of α‐iminophosphonates, enabling the efficient synthesis of chiral α‐aminophosphonates. Both acyclic and cyclic substrates are converted in high yields (up to 97%) with excellent enantioselectivities (up to >99:1), offering a practical alternative to conventional AH for accessing phosphorus‐containing chiral amines.