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.
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.
出处
《江南大学学报（自然科学版）》
CAS
2004年第6期611-613,共3页
Joural of Jiangnan University (Natural Science Edition)
关键词
唑来膦酸
四丁基碘化铵
合成
zoledronic acid
tetrabutyl ammonium iodide
synthesis
