芳亚甲基硝基缩氨基胍类化合物的合成及杀虫活性

依据活性亚结构拼接原理, 以硝基胍为原料, 合成了一系列具有新烟碱类和缩氨基脲类杀虫剂共同结构特征的芳亚甲基硝基缩氨基胍类化合物, 其结构通过¹H NMR、 IR和元素分析等方法进行了确证. 杀虫活性测定结果表明, 在600 μg/mL浓度下, 目标化合物对桃蚜Myzuspersicae(Sulzer)]具有较优异的活性, 其中化合物4-2, 4-8, 4-10, 4-16, 4-27, 4-31和4-34的校正死亡率均在90%以上. 进一步以桃蚜、 棉蚜(Aphis gossypii)和桃粉蚜(Hyalopterusamygdali blanchard)为对象, 测定了化合物4-2, 4-8和4-34的精密毒力. 结果表明, 它们在低浓度下仍然具有很高的活性, 其中化合物4-8对棉蚜的活性甚至优于对照药剂吡虫啉, 在3.13 μg/mL浓度下致死率仍高达95.7%(吡虫啉为79.4%), 具有进一步研究开发的价值.

Syntheses and Insecticidal Activities of Nitro Arylideneamino Guanidine Derivatives†

In order to search for better lead compounds with excellent biological activities, a novel series of acyclic neonicotinoids of nitro arylideneamino guanidine derivatives was designed and synthesized from nitroaminoguanidine by the method of linking the active substructures of neonicotiniod insecticides and semicarbazone insecticides. All the target compounds were confirmed by ¹H NMR, IR and elemental analysis. The preliminary bioassay showed that the lethal rates of target compounds to Myzuspersicae were excellent at the concentration of 600 μg/mL. The lethal rates of several compounds, such as 4-2, 4-8, 4-10, 4-16, 4-27, 4-31 and 4-34, were more than 90%. Further research of compounds 4-2, 4-8 and 4-34 against Myzuspersicae, Aphis gossypii and Hyalopterusamygdali blanchard indicated these compounds possessed high activity at low concentrations, especially, the activity of compound 4-8 was better than that of imidacloprid against Hyalopteraamygdali blanchard, its lethal rate was 95.7% compared to imidacloprid(79.4%) at the concentration of 3.13 μg/mL, which confirmed that this compound is worth of research.