| 唑来膦酸的工业合成 |
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| 引用本文： | 徐桂清,李富志,郝二军,韩凌,袁明贵,李伟. 唑来膦酸的工业合成[J]. 河南师范大学学报(自然科学版), 2009, 37(5) |
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| 作者姓名： | 徐桂清 李富志 郝二军 韩凌 袁明贵 李伟 |
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| 作者单位： | 河南师范大学,化学与环境科学学院,河南,新乡453007;河南天方药业股份有限公司,河南,驻马店,463000 |
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| 基金项目： | 河南省科技攻关计划项目，河南师范大学青年科学基金 |
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| 摘 要： | 以咪唑为起始原料,和氯乙酸乙酯经N-烷基化、水解、成盐得2-(1-咪唑基)乙酸盐酸盐(4),4再与磷酸、三氯化磷反应,然后精制得唑来膦酸(1),总收率为30.4%.合成的目标化合1,其结构经核磁共振氢谱、红外光谱、质谱及元素分析确证.与文献相比,改进后的路线操作简便,易于工业化,制得的产品纯度高.
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| 关 键 词： | 唑来膦酸 工业合成 咪唑 氯乙酸乙酯 |
Industrial Synthesis of Zoledronic Acid |
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| XU Gui-qing,LI Fu-zhi,HAO Er-jun,HAN Ling,YUAN Ming-gui,LI Wei. Industrial Synthesis of Zoledronic Acid[J]. Journal of Henan Normal University(Natural Science), 2009, 37(5) |
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| Authors: | XU Gui-qing LI Fu-zhi HAO Er-jun HAN Ling YUAN Ming-gui LI Wei |
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| Abstract: | Zoledronic acid is prepared from imidazole via N-alkylation with ethyl bromoacetate,followed by hydrolysis and salification to give 2-(1-imidazoly) acetic acid hydrochloride which is reacted with phosphoric acid and PCl3 to give the target compound.The overall yield is 30.4%.The structure of the target compound is confirmed by 1H-NMR、IR、MS and elemental analysis.Compared with the literature process,the improved method is more convenient and the purity of zoledronic acid is more than 99%. |
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| Keywords: | zoledronic acid industrial synthesis imidazole ethyl chloroacetate |
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