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[摘要]
目的 对阿哌沙班的合成工艺进行改进研究。方法 以4,5,6,7-四氢-1-(4-甲氧基苯基)-6-(4-硝基苯基)-7-氧代-1H-吡唑并[3,4-C]吡啶-3-羧酸乙酯为起始原料,通过还原、取代、环合、胺化反应得到阿哌沙班。结果 合成了目标化合物阿哌沙班,经MS、1H-NMR确证了结构,质量分数为99.2%,本合成工艺的总收率为76.4%。结论 该合成工艺改进后操作简单、安全,适合工业化生产。
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[Abstract]
Objective To study the improved method for synthesis of apixaban. Methods 4,5,6,7-Tetrahydro-1-(4-methoxyphenyl)-6-(4-nitrophenyl)-7-oxo-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester was used as starting material to synthesize apixaban by reduction reaction, substitution reaction, cyclization reaction, and amination reaction. Results The target compound apixaban was synthesized and characterized by MS and 1H-NMR. And the purity was 99.2%, and the total yield of this route was 76.4%. Conclusion The synthetic process has the advantages of simple operation, security, and suitable for industrial production.
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