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唑来膦酸的合成方法改进
An Improved Synthesis of Zoledronic Acid
【摘要】 通过两步反应合成得到唑来膦酸:咪唑和溴乙酸乙酯在相转移催化剂四丁基碘化铵作用下合成1H 咪唑 1 乙酸乙酯,直接水解制得1H 咪唑 1 乙酸;1H 咪唑 1 乙酸和三氯化磷、磷酸反应后再水解制得唑来膦酸.该方法操作简便,适用于工业化生产.通过元素分析、红外光谱、质谱和核磁共振谱对唑来膦酸进行了确认.
【Abstract】 Zoledronic acid is synthesized by two-step reactions. Ethyl 1H-imidazol-ylacetate is synthesized by reaction of imidazole with ethyl bromoacetate in the presence of tetrabutyl ammonium iodide, which is hydrolyzed directly to give 1H-imidazol-1-ylacetic acid. Zoledronic acid is gained by hydrolysis after reaction of 1H-imidazol-1-ylacetic acid with phosphorus trichloride and phosphoric acid . The process of synthesis is convenient and simple,and suitable for pharmaceutical industry.Zoledronic acid is identified by elementary analysis,IR,MS and NMR.
- 【文献出处】 江南大学学报 ,Journal of Southern Yangtze University , 编辑部邮箱 ,2004年06期
- 【分类号】R914
- 【被引频次】12
- 【下载频次】401