高等学校化学学报

高等学校化学学报

• 有机化学 • 上一篇    下一篇

新型喹唑啉酮衍生物的合成

唐健红1,2, 史大昕1, 王秀珍1, 刘璇1, 李加荣1   

  1. 1. 北京理工大学化工与环境学院, 北京 100081;
    2. 华侨大学化工学院, 厦门 361021
  • 收稿日期:2011-04-25 发布日期:2012-02-16
  • 通讯作者: 李加荣, 男, 博士, 教授, 博士生导师, 主要从事有机合成研究. E-mail:jrli@bit.edu.cn

Synthesis of Novel Quinazolinone Derivatives

TANG Jian-Hong1,2, SHI Da-Xin1, WANG Xiu-Zhen1, LIU Xuan1, LI Jia-Rong1   

  1. 1. School of Chemical Engineering and Environment, Beijing Institute of Technology, Beijing 100081, China;
    2. College of Chemical Engineering, Huaqiao University, Xiamen 361021, China
  • Received:2011-04-25 Published:2012-02-16

PDF (PC)

被引次数

8

摘要：

以醛、 丙二腈和酮为起始原料, 在乙酸铵的催化下一锅合成了2,6-二氰基苯胺衍生物3, 化合物3在NaOH催化下, 与酮经过分子内Pinner反应到Dimroth重排组合转化, 得到新型多取代喹唑啉酮衍生物5. 化合物5的结构经IR, 1H NMR, 13C NMR和MS表征. 喹唑啉酮衍生物是一系列药物的重要中间体.

关键词: 丙二腈, 2,6-二氰基苯胺衍生物, 喹唑啉酮, 环缩合

Abstract:

2,6-Dicyanoaniline derivatives(3) were synthesized from the multi-component condensation of aldehyde, malononitrile and ketone under the catalysis of ammonium acetate. Then 2,6-dicyanoaniline derivatives reacted with ketones to give mutli-substituted quinazolinone derivatives(5) using sodium hydroxide as catalyst at 100 ℃ or refluxing through intermolecule Pinner reaction via Dimroth rearrangement. The structures of the synthetic compounds were characterized by IR, 1H NMR, 13C NMR and MS. Quinazolinone derivatives are the important inter-mediate of a series of drugs.

Key words: Malononitrile, 2,6-Dicyanoaniline derivative, Quinazolinone, Cyclocondensation

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