新型硝基亚甲基类新烟碱化合物的合成及其杀虫活性

Synthesis and Insecticidal Activity of Novel Nitromethylene-containing Compounds

以昆虫乙酰胆碱受体为作用靶标的新烟碱类杀虫剂属于高效、高选择性和环境友好的杀虫剂,依据新烟碱类杀虫剂活性与结构关系,以吡虫啉及其类似物NTN32692为先导结构,在咪唑啉环位置并入可以增强分子脂溶性的六元环基团,设计合成了9个未见文献报道的硝基亚甲基类新烟碱化合物,所有目标化合物的结构均经1H NMR、IR和HR-MS测试技术的确证。初步的生物活性测试结果表明,在500 mg/L下所有目标化合物对豆蚜(Aphis craccivora)都有一定的杀死活性,其中活性最高的化合物4对豆蚜(Aphis craccivora)的校正死亡率为73.0%。并对目标化合物5a～5h的合成方法进行了探讨。

Neonicotinoid-insecticides are the inhibitors of insect nAChRs with higher herbicidal activity, higher degree of selectivity, and excellent environmental safety. Based on the relationship between structure and activity of nitromethylene heterocycle compounds, and using imidacloprid and its analogues NTN32692 as a model, new compounds which contain the framework of imidacloprid linking cyclohexane were synthesized and characterized with 1H NMR, IR and HR-MS. The bioassay indicates that nine nitromethylene heterocycle compounds have certain insecticidal activities against Aphis craccivora at 500 mg/L and the best one is 73%.