有机化学 ›› 2009, Vol. 29 ›› Issue (06): 962-965. 上一篇    下一篇

研究简报

无溶剂研磨合成6-氨基-8-芳基-2-甲基-5,7,7(1H)-三腈基-2,3,8,8a- 四氢异喹啉衍生物

荣良策*,a,b ; 韩红霞a ; 姜 虹b ; 庄启亚a ; 王苏惠a ; 屠树江a,b   

  1. (a徐州师范大学化学化工学院 徐州 221116)
    (b江苏省药用植物生物技术重点实验室 徐州 221116)
  • 收稿日期:2008-05-13 修回日期:2008-12-28 发布日期:2009-06-20
  • 通讯作者: 荣良策

Synthesis of 6-Amino-8-aryl-2-methyl-5,7,7(1H)-tricarbonitrile-2,3,8,8a- tetrahydroisoquinoline Derivatives under Solvent-Free Conditions Using a Ginding Method

Rong, Liangce*,a,b ; Han, Hongxiaa; Jiang, Hongb; Zhuang, Qiya a;
Wang, Suhuia; Tu, Shujiang a,b
  

  1. (a College of Chemistry and Chemical Engineering, Xuzhou Normal University, Xuzhou 221116)
    (b Key Laboratory of Biotechnology for Medicinal Plant, Xuzhou 221116)
  • Received:2008-05-13 Revised:2008-12-28 Published:2009-06-20
  • Contact: Rong, Liangce

NaOH存在下, 无溶剂室温研磨芳醛、丙二腈、N-甲基哌啶-4-酮, 方便地合成了一系列6-氨基-8-芳基-2-甲 基-5,7,7(1H)-三腈基-2,3,8,8a-四氢异喹啉衍生物, 该反应产率高, 操作简单. 所有产物的结构均经IR, 1H NMR, 元素分析进行了表征, 并采用X-ray晶体衍射分析进一步确定了产物4d的结构.

关键词: 研磨, 丙二腈, N-甲基哌啶-4-酮, 无溶剂, 芳醛

A series of 6-amino-8-aryl-2-methyl-5,7,7(1H)-tricarbonitrile-2,3,8,8a-tetrahydroisoquinoline derivatives were synthesized from aromatic aldehydes, malononitrile and N-methylpiperidin-4-one in the presence of sodium hydroxide under a solvent-free condition. The advantages of this procedure were simple protocol and high yields. The structures of products were determined by IR, 1H NMR spectra, elemental analysis, and 4d was additionally confirmed by X-ray diffraction analysis .

Key words: malononitrile, grinding, N-methylpiperidin-4-one, solvent-free, aromatic aldehyde