一种嘧啶联吡啶类化合物的合成研究

A synthetic study on the pyridinylpyrimidine compounds

开发了一种三乙胺促进的(E)-3-乙氧基-2-(吡啶-2-基)丙烯酸甲酯和甲基异硫脲缩合反应构建嘧啶联吡啶类骨架的新方法。以此反应为基础,经氯代和两步取代反应,最终合成了具有受体酪氨酸激酶抑制剂活性化合物(1r,4r)-4-((2-(丁基胺)-5-(吡啶-2-基)-嘧啶-4-基)胺)环己醇。该方法高效、简便且收率高。

A novel approach to construct pyridinylpyrimidine framework by trimethylamine promoted condensation of methyl（E ）-3 - ethoxy-2-（ pyridin-2-yl） acrylate and methyl carbamimidothioate had been developed. Through subsequent chlorination and SNAr re-actions,the synthesis of（ lr,4r） （ 2-（ butylamino）-5-（ pyridin-2-yl） pyrimidin^l-yl） amino） cyclohexan-l-ol as a receptor tyro-sine kinase inhibitor was achieved. This method was efficient,facile,and high-yielding.