有机化学 ›› 2008, Vol. 28 ›› Issue (9): 1637-1640. 上一篇    下一篇

研究简报

3-氨甲基-4-三氟甲基吡啶的合成研究

李 杰; 陈 浩; 周 勋; 陆秀宏 ; 陈国良*   

  1. (沈阳药科大学制药工程学院 沈阳 110016)
  • 收稿日期:2008-01-20 修回日期:2008-03-06 发布日期:2008-09-20
  • 通讯作者: 陈国良

Synthesis of 3-Aminomethyl-4-trifluoromethylpyridine

LI, Jie; CHEN, Hao; ZHOU, Xun; LU, Xiu-Hong ;CHEN, Guo-Liang*   

  1. (School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016)
  • Received:2008-01-20 Revised:2008-03-06 Published:2008-09-20
  • Contact: CHEN, Guo-Liang

以4,4,4-三氟乙酰乙酸乙酯与氰基乙酰胺为起始原料, 经环合、氯化、催化氢解和还原四步反应高纯度、高收率地得到了3-氨甲基-4-三氟甲基吡啶. 改进后的合成方法具有低成本、分离纯化容易、设备要求低等优点, 适合工业化生产.

关键词: 4,4,4-三氟乙酰乙酸乙酯, 3-氨甲基-4-三氟甲基吡啶, 合成

A new convenient synthesis of 3-aminomethyl-4-trifluoromethylpyridine using 4,4,4-trifluoroa- cetoacetate and cyanoacetamide as precursors, via cyclization, chlorination, hydrogenolysis and hydrogenation under mild conditions, was achieved. In comparison with other methods, there are some advantages in this method: low-cost, easy purification, low equipment requirements and suitability for industrial scale-up.

Key words: 4,4,4-trifluoroacetoacetate, synthesis, 3-aminomethyl-4-trifluoromethylpyridine