Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (08): 1385-1392. Previous Articles     Next Articles

Original Articles


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

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