伊班膦酸钠的合成研究

Study on the synthesis of sodium ibandronate

以正戊胺为起始原料合成了N-甲基正戊胺(3),化合物(3)与丙烯酸甲酯经过缩合和水解制得3-(N-甲基戊胺基)-丙酸盐酸盐(2),化合物(2)在无溶剂的情况下膦酸化和中和反应合成了伊班膦酸钠(1),总收率36.6%,其产品结构经1H NMRI、R、MS表征。该工艺具有原料易得,收率高,质量好,对环境污染小等特点。

Sodium ibandronate（1） in total yield of 36.6% was synthesized in without solvent by phosphorylation and neutralization of 3-（N-methylentylamino）propionic acid hydrochloride（2） which was prepared by condensation and hydrolysis from methyl acrylate with N-methylpentylamine（3） produced by the reaction of pentyamine.The structure of（1） was confirmed by 1H NMR,IR,MS.It has characteristics of ready availability of reactant,high yield,good quality,little pollution to environment.