| 利塞膦酸钠的合成研究 |
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| 引用本文： | 张秀立,张宇佳,王璐璐,方夏琴,陈少华,相莉,刘盟盟,郑稳生.利塞膦酸钠的合成研究[J].药学实践杂志,2013,31(6):448-450. |
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| 作者姓名： | 张秀立 张宇佳 王璐璐 方夏琴 陈少华 相莉 刘盟盟 郑稳生 |
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| 作者单位： | 中国医学科学院药物研究所,药物传输技术及新型制剂北京市重点实验室,北京100050 |
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| 摘 要： | 目的合成新型抗骨质疏松药利塞膦酸钠。方法以烟酸为原料，经酯化、缩合、Willgerodt反应和水解等步骤得到关键中间体3-吡啶乙酸盐酸盐，3-吡啶乙酸盐酸盐与亚磷酸反应后得到利塞膦酸钠。结果在合成过程中，通过探讨Willgerodt反应的时间和反应条件以及产率，优化合成路线，提高总反应收率。结论此合成路线使利塞膦酸钠的合成方法能较好地适用于工业化生产。
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| 关 键 词： | 利塞膦酸钠 抗骨质疏松药 化学合成 |
| 收稿时间： | 2012/12/27 0:00:00 |
| 修稿时间： | 2013/5/20 0:00:00 |
Synthesis of risedronate sodium |
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| ZHANG Xiu-li,ZHANG Yu-ji,WANG Lu-lu,FANG Xia-qin,CHEN Shao-hu,XIANG Li,LIU Meng-meng and ZHENG Wen-sheng.Synthesis of risedronate sodium[J].The Journal of Pharmaceutical Practice,2013,31(6):448-450. |
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| Authors: | ZHANG Xiu-li ZHANG Yu-ji WANG Lu-lu FANG Xia-qin CHEN Shao-hu XIANG Li LIU Meng-meng and ZHENG Wen-sheng |
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| Institution: | ( Institute of Materia Medica, Chinese Academy of Medical Sciences,Beijing City Key Laboratory of Drug Delivery Technology and Novel Formulations, Beijing 100050, China) |
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| Abstract: | Objective To synthesis the new anti - osteoporotic risedronate sodium. Methods Nicotinic acid was used as raw material, by esterification, condensation, Willgerodt reaction and hydrolysis steps to get the key intermediate 3-pyridine acetic acid hydrochloride. Then 3-pyridine acetic acid hydrochloride and phosphorous acid reacted to obtain the risedronate sodium. Results The reaction time, reaction conditions and the yield of Willgerodt reaction were explored. The synthetic route was optimized and the total yield of the reactions was increased. Conclusion This synthetic route of risedronate sodium could be applied to industrial production. |
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| Keywords: | risedronate sodium anti-osteoporotic chemical synthesis |
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