| 富马酸卢帕他定的合成 |
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| 引用本文： | 李六林,陈黎,盛荣. 富马酸卢帕他定的合成[J]. 中国现代应用药学, 2014, 31(12): 1481-1483 |
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| 作者姓名： | 李六林 陈黎 盛荣 |
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| 作者单位： | 浙江大学药学院，杭州 310058；浙江赐富医药有限公司，浙江 绍兴 312073;浙江赐富医药有限公司，浙江 绍兴 312073;浙江大学药学院，杭州 310058 |
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| 摘 要： | 目的 合成富马酸卢帕他定并改进工艺。方法 以5-甲基烟酸为起始物料，经过酯化、还原、氯化、烷基化、成盐等步骤制得富马酸卢帕他定。结果 所得产物经核磁共振氢谱、质谱、红外等确证其结构，总收率为46.4%。结论 该工艺安全可靠，方法简便，适合工业化生产。
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| 关 键 词： | 富马酸卢帕他定；5-甲基-3-吡啶甲醇；合成 |
| 收稿时间： | 2014-03-05 |
| 修稿时间： | 2014-06-10 |
Synthesis of Rupatadine fumarate |
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| LI Liulin,CHEN Li and SHENG Rong. Synthesis of Rupatadine fumarate[J]. The Chinese Journal of Modern Applied Pharmacy, 2014, 31(12): 1481-1483 |
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| Authors: | LI Liulin CHEN Li SHENG Rong |
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| Affiliation: | College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China; Zhejiang Cifu Pharmaceutical Co., Ltd., Zhejiang Shaoxing 312073, China;Zhejiang Cifu Pharmaceutical Co., Ltd., Zhejiang Shaoxing 312073, China;College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058 |
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| Abstract: | OBJECTIVE To synthesis rupatadine fumarate and optimize the reaction conditions. METHODS Rupatadine fumarate was synthesized from 5-methyl nicotinic via esterification, reduction, chlorination, alkylation and salification. RESULTS The rupatadine fumarate was synthesized with a total yield of 46.4% and its structure was confirmed by 1H-NMR, MS and IR. CONCLUSION The synthetic route is suitable for production of rupatadine fumarate in industry. |
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| Keywords: | rupatadine fumarate 5-methyl-3-pyridyl methanol synthesis |
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