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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。 |
| 关键词: 工艺改进 甲基化 还原 扎鲁司特 |
| DOI： |
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| Improved Synthetic Procedure of Zafirlukast |
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WU Xiaoguo, MAO Yaqin
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| Abstract: |
| OBJECTIVE To improve the synthetic procedure of zafirlukast．METHODS Zafirlukast was synthesized from 5-nitro-1H-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. |
| Key words: improved synthetic procedure methylation reduction zafirlukast |
