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制备N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺的方法

申请公布号:CN102199146A

申请号:CN201010129525.7

申请日期:2010.03.22

申请公布日期:2011.09.28

申请人:
上海希迪制药有限公司

发明人:刘蔚;吕峰;李迅

分类号:C07D401/14(2006.01)I

主分类号:C07D401/14(2006.01)I

代理机构:
上海专利商标事务所有限公司 31100

代理人:樊云飞

地址:201203 上海市浦东新区张江高科技园区张衡路1999号9号楼

摘要:本发明公开了一种N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺的制备方法。本发明的制备方法包括如下步骤:(a)在酯类溶剂中,在选自钯炭/甲酸铵、钯炭/甲酸、或钯炭/甲酸铵/甲酸的还原试剂的作用下,将N-(5-硝基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺进行还原;(b)从反应液中收集得到N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺。用本发明方法得到的产品收率可达90%以上,HPLC检测纯度可达99.5%以上。本发明方法工艺操作易控制,适合工业化生产。

主权项:一种N‑(5‑氨基‑2‑甲基苯基)‑4‑(3‑吡啶基)‑2‑嘧啶胺的制备方法,其特征在于,包括如下步骤:(a)在酯类溶剂中,在选自钯炭/甲酸铵、钯炭/甲酸、或钯炭/甲酸铵/甲酸的还原试剂的作用下,将N‑(5‑硝基‑2‑甲基苯基)‑4‑(3‑吡啶基)‑2‑嘧啶胺进行还原;(b)从反应液中收集得到N‑(5‑氨基‑2‑甲基苯基)‑4‑(3‑吡啶基)‑2‑嘧啶胺。

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