| 高血钙症治疗药唑来膦酸的合成方法改进 |
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| 引用本文： | 李家明,童元峰,张永. 高血钙症治疗药唑来膦酸的合成方法改进[J]. 中国药物化学杂志, 2002, 12(3): 164-165,186 |
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| 作者姓名： | 李家明 童元峰 张永 |
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| 作者单位： | 1. 安徽中医学院药物化学教研室,安徽,合肥,230038
2. 合肥医工医药研究所,安徽,合肥,230031 |
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| 摘 要： | 以咪唑为起始原料，与溴乙酸乙酯反应再经水解制得咪唑－1－基乙酸 ，最后与三氯化磷和亚磷酸反应经精制得到唑来膦酸，总收率为27．0％。在合成中使用TEBA替代BBDE Cl作为相转移催化剂、以咪唑乙酸替代咪唑乙酸盐酸盐进行反应，可以方便地得到纯度、收率均较好的产品。
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| 关 键 词： | 唑来膦酸 高血钙症 合成 |
| 文章编号： | 1005-0108(2002)03-0164-02 |
An improved synthesis of zoledronic acid as a new treating hypercalcemia drug |
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| LI Jia ming ,TONG Yuan feng ,ZHANG Yong. An improved synthesis of zoledronic acid as a new treating hypercalcemia drug[J]. Chinese Journal of Medicinal Chemistry, 2002, 12(3): 164-165,186 |
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| Authors: | LI Jia ming TONG Yuan feng ZHANG Yong |
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| Affiliation: | LI Jia ming 1,TONG Yuan feng 2,ZHANG Yong 2 |
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| Abstract: | Zoledronic acid,a new drug for treating hypercalcemia,was synthesized by the condensation of imidazole with ethyl bromoacetate,hydrolysis to afford imidazole 1 ylacetic acid,and then reacted with phosphorous acid and phosphorus trichloride to give the target product,the overall yield was 27 0%.In this paper,we used TEBA instead of BBDE Cl as phase transfer catalyst,and imidazole acetic acid instead of its hydrochloride salt as the key intermediate,this process can easily obtain the product in good quality and yield. |
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| Keywords: | zoledronic acid hypercalcemia synthesis |
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