Preparation d'acides aminoalkyl phosphoniques a l'aide d'ω-halogenoalkyl amines phosphorylees
作者:D. Brigot、N. Collignon、Ph. Savignac
DOI:10.1016/0040-4020(79)85028-0
日期:1979.1
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。