2-Phenyl-1H-pyrrolo[2,3-b]pyridine was synthesized from 3-methyl pyridine and benzonitrile. Then,the structure of a-crylic acid compound was obtained by substitution reaction with methyl iodide,DMF,and malonic acid,successively. Finally,SIS3 (small molecule inhibitors of Smad3)was obtained through condensation and salt formation with an overall yield of about 40%.The structure of the product was confirmed by 1 H NMR and MS. This method had advantages of mild reaction conditions,high yield,and convenient purification.%以3-甲基吡啶和苯甲腈为原料反应得到2-苯基-1H-吡咯并[2，3-b]吡啶，再通过与碘甲烷、DMF和丙二酸反应得到具有丙烯酸结构的化合物，最后通过缩合、成盐，制备获得了Smad3小分子抑制剂SIS3。产物总收率达40％。产物经1 H NMR和MS分析确认。此方法具有反应条件温和、产率高、产品易纯化等特点。
展开▼
