扎鲁司特的合成工艺改进

Improved Synthetic Procedure of Zafirlukast

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。

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.