阿仑膦酸钠的合成

Synthesis of alendronate sodium trihydrate

目的:探讨抗骨质疏松药阿仑磷酸钠的合成。方法:以γ-氨基丁酸(gamma-aminobutyric acid,GABA)、亚磷酸、三氯化磷为原料,采用二苯醚作溶剂制备阿仑磷酸,再经中和、碱化制得阿仑磷酸钠盐。结果:得到白色晶状产物,熔点测试与核磁共振谱显示其正确无误。两步收率分别为78.5%和83.6%。结论:本工艺适合于工业化生产。

Objective：To synthesize anti-osteoporosis drug sodium alendronate.Methods：By using gamma-aminobutyric acid（GABA）,phosphorous acid and phosphorus trichloride as the raw materials,and diphenyl ether as solvent to prepare alendronate phosphoric acid.Sodium alendronate was obtained through neutralization and alkalization.Results：The white crystalline product was identified by melting point and nuclear magnetic resonance.The yield of the two steps reached 78.5% and 83.6% respectively.Conclusion：The procedure is suitable for industrialized production.