有机化学 ›› 2012, Vol. 32 ›› Issue (07): 1303-1307.DOI: 10.6023/cjoc1111011 上一篇    下一篇

研究论文

新型双吲哚马来酰亚胺衍生物的合成

方勇波, 李丽秀, 卢杏萍, 黎金海, 黄雁   

  1. 广州医学院基础学院 广州 510182
  • 收稿日期:2011-11-01 修回日期:2012-01-19 发布日期:2012-03-09
  • 通讯作者: 黄雁 E-mail:drhuangyan@163.com
  • 基金资助:
    广东省科技计划(No. 2008B060600074)及广州市属高校科技计划(No. 08A107)资助项目.

Synthesis of Novel Bisindolylmaleimide Derivatives

Fang Yongbo, Li Lixiu, Lu Xingping, Li Jinhai, Huang Yan   

  1. School of Basic Science, Guangzhou Medical College, Guangzhou 510182
  • Received:2011-11-01 Revised:2012-01-19 Published:2012-03-09
  • Supported by:
    Project supported by the Guangdong Provincial Program of Science and Technology (No. 2008B060600074) and the Guangzhou Municipal University Program of Science and Technology (No. 08A107).

以1-(3-氧代四氢吡喃丙基)-吲哚-3-乙醛酸甲酯5和吲哚-3-乙酰胺6为原料, 在催化剂叔丁醇钾的四氢呋喃溶液存在下发生偶合反应, 经浓盐酸处理得脱保护的中间体7, 再经甲磺酰化反应、氨解反应得到4 种新的具有不同氨烷基侧链的双吲哚马来酰亚胺衍生物9a, 9b, 9d, 9e. 目标产物结构通过1H NMR, 13C NMR, MS 和HRMS 确证.

关键词: 双吲哚马来酰亚胺, 衍生物, 合成

Four novel bisindolylmaleimides 9a,9b,9d,9e containing different aminoalkyl side chains were derived from methylsulfonylation, ammonolysis of the intermediate 7, which was prepared by reaction of methyl[1-(3-O’-tetrahydropyranepropyl)indolyl-3]-glyoxylate (5) with indole-3-acetamides (6) using t-BuOK in THF as catalyst and treatment using concentrated hydrochloric acid subsequently.The structures of target products were also confirmed by 1H NMR,13C NMR, MS,HRMS techniques.

Key words: Bisindolylmaleimide, Derivatives, Synthesis