一种嘧啶联吡啶类化合物的合成研究

摘要

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 reactions,the synthesis of(1 r,4r)-4-((2-(butylamino)-5-(pyridin-2-yl) pyrimidin-4-yl) amino) cyclohexan-1-ol as a receptor tyrosine kinase inhibitor was achieved.This method was efficient,facile,and high-yielding.