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新型2-芳氨基嘧啶衍生物的合成
引用本文:马大友,余聂芳.新型2-芳氨基嘧啶衍生物的合成[J].有机化学,2008,28(8):1448-1453.
作者姓名:马大友  余聂芳
作者单位:中南大学药学院,长沙,410013
基金项目:中南大学升华学者基金,国家自然科学基金,中国博士后科学基金
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, 1H NMR, 13C NMR, MS和元素分析表征而予以证实.

关 键 词:Pd(PPh3)4  dppf  2-芳氨基嘧啶  偶联反应
收稿时间:2007-9-17
修稿时间:2007-12-14

Synthesis of Novel 2-(Substituted anilino)pyrimidine Derivatives
MA,Da-You,YU,Nie-Fang.Synthesis of Novel 2-(Substituted anilino)pyrimidine Derivatives[J].Chinese Journal of Organic Chemistry,2008,28(8):1448-1453.
Authors:MA  Da-You  YU  Nie-Fang
Institution:School of Pharmacy, Central South University, Changsha 410013
Abstract: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.
Keywords:Pd(PPh3)4  dppf
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