| 拉奎莫德的合成工艺优化 |
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| 引用本文： | 郑赫宏,陈国华,陆建军.拉奎莫德的合成工艺优化[J].安徽医药,2013,17(5):745-746. |
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| 作者姓名： | 郑赫宏 陈国华 陆建军 |
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| 作者单位： | 中国药科大学药物化学教研室,江苏,南京,210009;中国药科大学药物化学教研室,江苏,南京,210009;中国药科大学药物化学教研室,江苏,南京,210009 |
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| 摘 要： | 目的分析比较拉奎莫德的合成方法并且进行工艺优化。方法以2-氨基-6-氯苯甲酸为起始原料与氯甲酸苄酯、乙酰氯进行环合反应,再经甲基化、缩合、酰胺化反应制得拉奎莫德。结果合成的拉奎莫德的总收率为77.8%,纯度为99.1%。其结构经1H-NMR和MS确证。结论工艺改进后,操作简化,成本降低,收率提高,适合工业化生产。
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| 关 键 词： | 拉奎莫德 2-氨基-6-氯苯甲酸 合成 |
Optimization of synthesis of.Laquinimod |
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| ZHENG He-hong,CHEN Guo-hua,LU Jian-jun.Optimization of synthesis of.Laquinimod[J].Anhui Medical and Pharmaceutical Journal,2013,17(5):745-746. |
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| Authors: | ZHENG He-hong CHEN Guo-hua LU Jian-jun |
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| Institution: | ( Department of Medicinal Chemistry, China Pharnuweutical Unlversity,Nanjing 210009, China) |
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| Abstract: | Objective To synthesize Laquinimod and optimize the synthetic technology. Methods Taking 2-amino-6-chlorobenzoic acid as raw material, Laquinimod was synthesized by a series of chemical reactions including cyclization, methylation, condensation, and amidation. Results Laquinimod was prepared with an overall rate of 77.8%. Conclusion The improved procedure could simplify the synthesis, reduce the cost and improve the yield. |
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| Keywords: | Laquinimod 2-amino-6-chorobenzoic acid synthesis |
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