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目的改进二氢乳清酸脱氢酶抑制剂特立氟胺的合成工艺。方法以氰乙酸和对三氟甲基苯胺为起始原料,采用一锅法制得中间体2-氰基-N-(4-三氟甲基苯基)乙酰胺,该中间体与乙酰氯反应制得目标化合物。结果与结论目标化合物的结构经~1H-NMR、~(13)C-NMR、MS谱确证。与文献报道的方法相比,该工艺路线提高了反应收率,降低了反应成本且反应条件温和,适合工业化生产,总收率为69.1%(以对三氟甲基苯胺计)。
Objective To improve the synthesis process of dihydroortantrine dehydrogenase inhibitor teriflunomide. Methods Cyanoacetic acid and p-trifluoromethylaniline were used as starting materials to prepare the intermediate 2-cyano-N- (4-trifluoromethylphenyl) acetamide in one pot. The intermediate was reacted with acetyl chloride The title compound was obtained. Results and Conclusion The structures of target compounds were confirmed by ~ 1H-NMR, ~ (13) C-NMR and MS spectra. Compared with the methods reported in the literature, the process route improves the reaction yield, reduces the reaction cost and the mild reaction conditions, and is suitable for industrial production. The total yield is 69.1% based on the trifluoromethylaniline.