摘要
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8h缩短至9min,且收率大大提高.同时,在250μg/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.
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 derivatives 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 microwave 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.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2008年第8期1385-1392,共8页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(Nos.20702018,20432010,20476036)
教育部跨世纪优秀人才、教育部重点科技项目(No.104205)
湖北省自然科学基金优秀群体(No.2004ABC002)资助项目
关键词
微波辅助组合合成
噻唑-4-酮
色酮
杀虫活性
microwave-assisted combinatorial synthesis
thiazolidinone
chromone
insecticidal activity
