Preparation d'acides aminoalkyl phosphoniques a l'aide d'ω-halogenoalkyl amines phosphorylees

Abstract

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 residue may be brought about by treatment with aqueous hydrogen chloride. Improvements in the isolation of the amino-phosphonic acids are described.