高等学校化学学报 ›› 2018, Vol. 39 ›› Issue (11): 2433.doi: 10.7503/cjcu20180215

• 有机化学 • 上一篇    下一篇

3-烷基膦酸酯基取代的异吲哚啉酮衍生物的合成及生物活性

刘笑宇, 徐议, 唐良富()   

  1. 南开大学化学学院, 元素有机化学国家重点实验室, 天津 300071
  • 收稿日期:2018-03-19 出版日期:2018-11-10 发布日期:2018-09-10
  • 作者简介:联系人简介: 唐良富, 男, 博士, 教授, 主要从事有机化学研究. E-mail: lftang@nankai.edu.cn
  • 基金资助:
    国家重点研发计划项目(批准号: 2017YFD0200900)资助.

Synthesis and Biological Activity of 3-Alkylphosphonate Substituted Isoindolinone Derivatives

LIU Xiaoyu, XU Yi, TANG Liangfu*()   

  1. State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China
  • Received:2018-03-19 Online:2018-11-10 Published:2018-09-10
  • Contact: TANG Liangfu E-mail:lftang@nankai.edu.cn
  • Supported by:
    † Supported by the National Key Research and Development Program of China(No.2017YFD0200900).

摘要:

通过邻溴芳香亚胺的锂化及与一氧化碳的环化反应, 随后与溴代烷基膦酸酯的“一锅法”反应, 合成了一系列3-烷基膦酸酯基取代的异吲哚啉酮衍生物. 利用核磁共振波谱及高分辨质谱对其结构进行了表征. 初步的生物活性测试结果表明, 部分化合物表现出明显的离体抗真菌活性.

关键词: 异吲哚啉酮, 膦酸酯, 亚胺, 抗真菌活性

Abstract:

A simple and convenient one-pot synthesis of 3-alkylphosphonate substituted isoindolinone derivatives via the reaction of o-lithiated aromatic imines with carbon monoxide under one atmospheric pressure followed with bromoalkyl phosphonate was developed. These newly synthesized 3-alkylphosphonate isoindolinones were characterized by 1H NMR, 13C NMR and 31P NMR as well as HRMS. Preliminary in vitro tests for fungicidal activity of these isoindolinone derivatives indicated that most of them exhibit good fungicidal activity.

Key words: Isoindolinone, Phosphate, Aromatic imine, Fungicidal activity

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