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

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.

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

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.