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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (08): 1448-1453. 上一篇    下一篇

研究简报

新型2-芳氨基嘧啶衍生物的合成

马大友 ; 余聂芳*   

  1. 中南大学药学院 长沙 410013
  • 收稿日期:2007-09-17 修回日期:2007-12-14 发布日期:2008-08-18
  • 通讯作者: 余聂芳

Synthesis of Novel 2-(Substituted anilino)pyrimidine Derivatives

MA, Da-You; YU, Nie-Fang*   

  1. School of Pharmacy, Central South University, Changsha 410013
  • Received:2007-09-17 Revised:2007-12-14 Published:2008-08-18
  • Contact: YU, Nie-Fang

PDF

724

被引次数

12

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, 1H NMR, 13C NMR, MS和元素分析表征而予以证实.

关键词: Pd(PPh3)4, dppf, 偶联反应, 2-芳氨基嘧啶

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.

Key words: dppf, 2-(substituted anilino)pyrimidine, coupling reaction, Pd(PPh3)4