【作者】 马臻； 王尊元； 沈正荣；

【Author】 MA Zhen, Wang Zun-Yuan, SHEN Zheng-Rong Zhejiang Academy of Medical Sciences, Hangzhou 310013

【机构】 浙江省医学科学院；

【摘要】 目的: 合成抗纤维化药物吡非尼酮。方法以2-氨基-5-甲基吡啶为起始原料,经重氮化、水解得到关键中间体5- 甲基-2(1H)吡啶酮,再与碘苯反应得到吡非尼酮。结果合成的吡非尼酮经熔点测定、红外光谱IR,核磁共振氢谱1H-NMR、质谱MS结构确证,总收率50．0％。结论合成路线简捷,工艺操作简化、环保,适于放大生产。更多还原

【Abstract】 OBJECTIVE To synthesize pirfinedone, a novel antifibrotic drug. METHODS Starting from 2-amino-5-methyl-pyridine, the key intermidiate 5-methyl-2(1H) pyridone was obtained via the way of diazotization, hydrolysis, then it was aromatized with iodobenzene to give pirfenidone. RESULTS The structure of pirfenidone was conformed by melting point, IR, 1HNMR. The overall yield of 50.0%. CONCLUSIONS The method was easy to operation.更多还原