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有机化学
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有机化学 ›› 2008, Vol. 28 ›› Issue (08): 1385-1392. 上一篇    下一篇

研究论文

微波辅助下N-酰胺基-2-(4-氧代-4H-色烯-3-基)噻唑-4-酮类衍生物的平行合成及其杀虫活性

周中振a,b ; 陈 琼*,a; 杨光富a   

  1. (a华中师范大学农药化学与生物学教育部重点实验室 武汉 430079)
    (b南方医科大学药学院 广州 510515)
  • 收稿日期:2007-11-15 修回日期:2008-01-09 发布日期:2008-08-18
  • 通讯作者: 陈 琼

Synthesis and Insecticidal Activities of N-Carbonylamido-2-(4-oxo- 4H-1-benzopyran-3-yl)-4-thiazolidinones Derivatives by Microwave-Assisted Parallel Syntheses

ZHOU, Zhong-Zhena,b ; CHEN, Qiong*,a ; YANG, Guang-Fua   

  1. (a Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, College of Chemistry,
    Central China Normal University, Wuhan 430079)
    (b School of Pharmaceutical Sciences, Southern Medical Universtiy, Guangzhou 510515)
  • Received:2007-11-15 Revised:2008-01-09 Published:2008-08-18
  • Contact: CHEN, Qiong

PDF

636

被引次数

37 | 8

利用微波辅助组合平行合成技术, 色酮酰腙类衍生物与巯基乙酸发生缩合反应, 成功地构建了N-酰胺基-2-(4-氧代-4H-色烯-3-基)噻唑-4-酮类化合物库. 与常规加热方法相比较, 反应时间由原来的8 h缩短至9 min, 且收率大大提高. 同时, 在250 μg/mL下, 检测了其杀虫活性, 初步生物测试结果表明部分化合物对红蜘蛛显示出良好的杀虫活性.

关键词: 微波辅助组合合成, 噻唑-4-酮, 杀虫活性, 色酮

A liquid-phase combinatorial synthesis of N-carbonylamido-2-(4-oxo-4H-1-benzopyran-3-yl)-4- thiazolidinones derivatives was successfully performed using N’-(chromon-3-yl)methylidene hydrazide de-rivatives and mercaptoacetic acid as reactants. Compared to an identical library generated by conventional parallel synthesis, the microwave-assisted parallel synthesis approach dramatically decreased the reaction time from an average of 8 h to 5 min, and substantially increased the product yields. The coupling of micro-wave technology with liquid-phase combinatorial synthesis constituted a novel and particularly attractive avenue for the rapid generation of structurally diverse libraries. At the same time, preliminary bioassay showed that part of them had insecticidal activities against Aphismedicagini at 250 μg•mL－1.

Key words: microwave-assisted combinatorial synthesis, chromone, insecticidal activity, thiazolidinone