一类具有良好杀虫活性的异噁唑啉类衍生物的合成

Synthesis of isoxazoline derivatives with good insecticidal activity

为开发出结构新颖,杀虫活性高,对环境友好型的杀虫剂,以商品化品种氟雷拉纳为先导化合物,对其结构尾链进行修饰。以4-溴-2-甲基苯甲酸为起始原料,经四步合成得到中间体V,设计并合成了14个未见文献报道的含三氟甲基的异噁唑啉结构的化合物,化合物及其中间体的化学结构均经^(1)H NMR和LC-MS确证。所合成的化合物经生物活性测试结果表明:化合物V-4、V-10、V-14在50 mg·L^(-1)的浓度下对小菜蛾(Plutella xylostella)的致死率均达百分之百。这为进一步合成杀虫活性较高的新型异噁唑啉类化合物提供参考。

In order to develop new insecticides with novel structure,high insecticidal activity and environmental friendliness,the tail chain of commercial variety flurana was modified.Using 4-bromo-2-methylbenzoic acid as starting material,an intermediate was synthesized via four steps.Twelve compounds with trifluoromethyl containing isoxazoline structure were designed and synthesized.The chemical structures of the compounds and their intermediates were confirmed by ^(1)HNMR and LC-MS.The results of biological activity test showed that the lethal rates of compounds V-4,V-10,V-14 to the third instar larvae of Plutella xylostella at the concentration of 50 mg·L^(-1) were 100%.This provided a reference for the further synthesis of new isoxazole compounds with high insecticidal activity.