利用类Mannich反应不对称合成N-磷酰氨基α-氨基膦酸单酯

convenient method has been developed for the diastereoselective synthesis of diisopropyl (R,R)-2-hydroxy-3-{(((R/S)-1-diethylphosphorylamido-1-arylmethyl) hydroxyphosphinyl)oxy}succin ate through Mannich-type reactions. The diastereoselectivity of the reaction using chiral reactant was investigated. The chiral 2-chloro-(4R,5R)-dicarboisopropoxy-1,3,2-dioxaphospholane 3 was found to be a good stereoselective phosphonylating agent towards this reaction.