新型2-芳氨基嘧啶衍生物的合成  

Synthesis of Novel 2-(Substituted anilino)pyrimidine Derivatives

作　　者：马大友[1] 余聂芳[1] 

机构地区：[1]中南大学药学院,长沙410013

出　　处：《有机化学》2008年第8期1448-1453,共6页Chinese Journal of Organic Chemistry

基　　金：中南大学升华学者基金;自然科学基金(No.30772645);中国博士后基金(No.20070410313)资助项目

摘　　要：通过间羟基苯硼酸与2,4-二氯嘧啶的Suzuki反应及其后酚羟基的烷基化得到4-芳基-2-氯嘧啶衍生物.然后,采用Pd(PPh3)4/dppf催化剂,在温和的条件下实现了4-芳基-2-氯嘧啶类化合物和芳香胺的偶联.合成了3个结构新颖的2-芳氨基嘧啶类化合物.中间体及产物的结构均经由IR,1HNMR,13CNMR,MS和元素分析表征而予以证实.4-（m-Substituted phenyl）-2-choloro-pyrimidines were prepared by Suzuki coupling reaction of 3-hydroxyphenylboronic acid with 2,4-dichloropyrimidine followed by alkylation of the hydroxyl group, which were effectively aminated by arylamine under catalysis of Pd（PPh3）4/dppf. Three novel 2- 2-（substituted anilino）pyrimidine derivatives were thus conveniently synthesized. The structures of all the synthesized compounds were fully characterized by IR, ^1H NMR, ^13C NMR, mass spectra and elemental analysis.

关 键 词：Pd(PPh3)4 DPPF 2-芳氨基嘧啶 偶联反应 

分 类 号：O626[理学—有机化学]