吡非尼酮的合成及结构确证

Synthesis and structural identification of Pirfenidone

目的合成抗纤维化药物吡非尼酮。方法以2-氨基-5-甲基吡啶为原料,经重氮化水解为5-甲基-2(1H)-吡啶酮,再经N-芳基化反应得到吡非尼酮。结果合成的吡非尼酮经高分辨质谱、紫外吸收光谱、红外吸收光谱、核磁共振谱、质谱和热分析确证结构,总收率为49.0%,纯度≥99.9%。结论该合成工艺操作简便,收率高,纯度高,是合成吡非尼酮的较好方法。

Objective To synthesize Pirfenidone, a novel antifibrotic drug. Methods Pirfenidone was synthesized from 2-amino-5-methylpyridin,via diazotization,hydrolysis,N-phenylation. Results The structure of Pirfenidone was confirmed by ESI-MS,UV,IR, NMR,MS,DSC and TGA. The total yield was 49. 0% and the purity of Pirfenidone ≥99. 9%. Conclusions The method is a better process with simple procedure,good yield and high purity.