| 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. |
| LI Liulin,CHEN Li,SHENG Rong.Synthesis of Rupatadine fumarate[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(12):1481-1483. |
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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。 |
| 关键词: 富马酸卢帕他定 5-甲基-3-吡啶甲醇 合成 |
| DOI： |
| 分类号:R284.1；R917.101 |
| 基金项目: |
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| Synthesis of Rupatadine fumarate |
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LI Liulin1,2, CHEN Li2, SHENG Rong3
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1.College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China;2.Zhejiang Cifu Pharmaceutical Co., Ltd., Zhejiang Shaoxing 312073, China;3.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. |
| Key words: rupatadine fumarate 5-methyl-3-pyridyl methanol synthesis |
