取代噻吩双酰胺类化合物的设计、合成及生物活性

Design,Synthesis and Biological Activity of Novel Substituted Diamides Derivatives Containing Thiophene Ring

利用中间体衍生化方法,将噻吩环引入到双酰胺类化合物中,合成了一系列取代噻吩双酰胺类化合物1-3;目标化合物的结构经核磁共振波谱、红外光谱及元素分析确认.生物活性测试结果表明,化合物1在600 mg/L剂量下对小菜蛾具有良好的杀虫效果,致死率均为100%,其中化合物1a和1e在20 mg/L剂量下对小菜蛾的致死率仍达到60%以上;改变双酰胺结构中的吡唑环得到化合物2和3,其杀虫活性消失,说明该类化合物中吡唑环结构对杀虫活性具有关键作用.

To discover novel diamide derivatives with high insecticidal activity,a series of new substituted diamide derivatives（ 1—3） containing thiophene ring was synthesized by introducing thiophene ring to diamide derivatives utilizing intermediate derivatization methods（ IDM）. The compounds were identified by1 H NMR,IR and elemental analysis. Preliminary bioassays indicated that compound 1 exhibited excellent insecticidal activities against Plutella xylostella and showed 100% mortality at 600 mg/L. Compounds 1a and 1e showed above 60% mortality at 20 mg/L. Compounds 2 and 3 attained by changing the pyrazole ring in diamide derivatives have no insecticidal activity,which illustrated that pyrazole ring in diamide derivatives is very important.