Ru‐Catalyzed Asymmetric Transfer Hydrogenation of α‐iminophosphonates: A Novel Synthetic Approach for Valuable Chiral α‐Aminophosphonates

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.