| 扎鲁司特的合成工艺改进 |
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| 引用本文： | 吴孝国,毛亚琴. 扎鲁司特的合成工艺改进[J]. 中国现代应用药学, 2009, 26(1): 36-38 |
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| 作者姓名： | 吴孝国 毛亚琴 |
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| 作者单位： | 浙江诚意药业有限公司，浙江 温州 325700 |
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| 摘 要： | 目的合成扎鲁司特，改进工艺。方法5-硝基-1H-吲哚经甲基化、付-克反应、缩合、还原和酰胺化反应制得扎鲁司特，主要对甲基化、付-克反应和还原工艺进行了改进。结果通过优化条件合成了扎鲁司特，总收率31．6％，目标化合物结构经红外、质谱、核磁共振谱、元素分析确证。结论改进后的工艺原材料价廉易得，降低了生产成本，更适合工业化生产。
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| 关 键 词： | 工艺改进 甲基化 还原 扎鲁司特 |
| 收稿时间： | 1900-01-01 |
Improved Synthetic Procedure of Zafirlukast |
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| WU Xiaoguo,MAO Yaqin. Improved Synthetic Procedure of Zafirlukast[J]. The Chinese Journal of Modern Applied Pharmacy, 2009, 26(1): 36-38 |
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| Authors: | WU Xiaoguo MAO Yaqin |
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| Affiliation: | Zhejiang Chengyi Pharmaceutical Co.,Ltd,Wenzhou 325700, China |
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| Abstract: | OBJECTIVE To improve the synthetic procedure of zafirlukast. METHODS Zafirlukast was synthesized from 5- nitro-lH-indole via methylation, alkylation, condensation, reduction and acylation. The methylation, alkylation and reduction are key steps in the procedure. RESULTS Zafirlukast was prepared in an overall yield of 31.6%. The structure of the target compound was confirmed by IR spectra, MS, H-NMR and elemental analysis. CONCLUSION The improved procedure avoids the use of expensive reagents and the target compound was synthesized in a convenient way. The method is suitable for industrial manufacture. |
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| Keywords: | improved synthetic procedure methylation reduction zafirlukast |
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