| 卢帕他定中间体5-甲基吡啶-3-羧酸的合成工艺改进 |
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| 引用本文： | 王震宇,朱雄,王尔华.卢帕他定中间体5-甲基吡啶-3-羧酸的合成工艺改进[J].药学进展,2005,29(1):31-33. |
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| 作者姓名： | 王震宇 朱雄 王尔华 |
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| 作者单位： | 中国药科大学医药化工研究所,江苏,南京,210009 |
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| 摘 要： | 目的:改进5-甲基吡啶-3-羧酸的合成工艺。方法:以3,5-二甲基吡啶为原料,经KMnO4氧化得卢帕他定中间体5-甲基吡啶-3-羧酸,经正交试验,优化工艺。结果:得出较佳的工艺条件,提高了产率,收率可达51％。结论:该方法易于工业化生产。
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| 关 键 词： | 3 5-二甲基吡啶 5-甲基吡啶-3-羧酸 氧化 正交试验 合成 |
| 文章编号： | 1001-5094(2005)01-0031-03 |
Improved Synthesis of 5-Methylpyridine-3-carboxylic Acid,the Intermediate of Rupatadine |
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| WANG Zhen-yu,ZHU Xiong,WANG Er-hua.Improved Synthesis of 5-Methylpyridine-3-carboxylic Acid,the Intermediate of Rupatadine[J].Progress in Pharmaceutical Sciences,2005,29(1):31-33. |
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| Authors: | WANG Zhen-yu ZHU Xiong WANG Er-hua |
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| Abstract: | Objective: To improve the synthesis of 5-methylpyridine-3-carboxylic acid. Methods: 5-methylpyridine-3-carboxylic acid, the intermediate of Rupatadine, was synthesized from 3,5-lutidine by the reaction of oxidation with KMnO4. The reaction conditions were optimized with the orthogonal matrix. Results: The suitable conditions were obtained, and the yield was 51 % . Conclusion: The process is practical and easy to popularize in industry. |
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| Keywords: | 3 5-Lutidine 5-Methylpyridine-3-carboxylic acid Oxidation Orthogonal test Synthesis |
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