Aminoalkylphosphonic acids are prepared via amino group protection by nitrogen-phosphorus (P-N) bond formation. Phosphorylation of β or γ-bromoalkylamines with chlorophosphates followed by reaction of the resulting haloalkylphosphoramidates with triethylphosphite (Arbuzov reaction) to give a phosphoramidate-phos-phonate intermediate which can be alkylated with various reagents. Removal of the phosphoryl
氨基烷基
膦酸是通过氮-
磷(
PN)键形成的
氨基保护基来制备的。β或γ-
溴代烷基胺用
氯磷酸盐进行
磷酸化,然后使所得卤代烷基膦酰胺化物与
亚磷酸三乙酯反应(Arbuzov反应),得到可以用各种试剂烷基化的
氨基
磷酸酯-
膦酸酯中间体。可以通过用
氯化氢水溶液处理来除去
磷酰基残基。描述了对
氨基膦酸的分离的改进。