α-氨基芳甲基膦酸二酯的制备

Preparation of Primary Dialkyl 1-Aminoarylmethylphosphonate

以苄胺、芳香醛和亚磷酸二乙酯为主要原料,经过类Mannich和催化氢化脱苄两步反应合成了系列的α-氨基芳甲基膦酸二乙酯,总产率可以达到70%—90%。该方法条件温和、简单、易于操作、适宜于规模化生产,为α-氨基芳甲基膦酸二酯的放大量生产奠定了基础。

An efficient method was reported for the synthesis of primary 1-Amino-arylmethylphosphonate via two-step reaction of Mannich-type reaction of aromatic aldehyde,benzylamine and diethyl phosphite,and subs-equently catalytic hydrogenizing debenzylation.By this method,a series of primary diethyl 1-aminoaryl methy-lphosphonates were prepared in good to excellent yields.This method is facile,easy to handle and suitable for large-scale production of primary dialkyl 1-amino-arylmethylphosphonate.