Nucleophilic addition of dimethyl phosphite to acylamino ketones prepared conveniently by the Dakin-West reaction involving reaction of the corresponding α-amino acids and acid anhydrides, followed by subsequent hydrolysis affords 1-alkyl(aryl)-2-amino-1-hydroxyalkylphosphonic acids in satisfactory yield.
将
亚磷酸二甲酯与通过达
金-韦斯特反应(涉及相应的δ-
氨基酸和酸酐的反应)方便地制备的酰
氨基酮进行亲核加成,然后进行
水解,就能以令人满意的收率得到 1-烷基(芳基)-2-
氨基-1-羟基烷基
膦酸。