Synthesis and Insecticidal Activities of Novel Analogues of Flubendiamide Containing a Hexafluoroisopropanol Moiety

Ten novel analogues of flubendiamide containing a hexafluoroisopropanol moiety were designed and synthe- sized. Their insecticidal activities against armyworm （Pseudaletia separata Walker） were examined and compared with the commercial product flubendiamide. Compound 7b showed nearly the same insecticidal activity as fluben- diamide against armyworm.

Design,synthesis and insecticidal activities of novel anthranilic diamides containing fluorinated groups as potential ryanodine receptors activitors

In order to search for novel potent and environmentally benign insecticides,a series of anthranilic diamides containing various fluorinated groups were designed and synthesized.Their structures were confirmed by -1H NMR,-（13）C NMR,-（19）F NMR,elemental analysis,HRMS or mass spectra.Their insecticidal activities against oriental armyworm（Mythimna separata） and diamondback moth（Plutella xyiostella）were evaluated.The preliminary structure-activity relationship（SAR） was discussed in detail.The biological assay indicated that most of the compounds exhibited moderate to excellent insecticidal activities.Especially,Ia showed high larvicidal activity against oriental armyworm.Meanwhile,Iu had better larvicidal effects against diamondback moth than commercial chlorantraniliprole.

含硫吡唑-4-酰胺类衍生物的设计、合成与生物活性

为寻找高生物活性的吡唑酰胺类化合物,在氯虫酰胺分子基础上,经结构优化,设计、合成一系列含硫结构的N-吡啶基吡唑-4-酰胺类衍生物,目标化合物经~1HNMR、CNMR、有机元素分析仪或高分辨质谱仪确证,并进行了初步杀虫及杀菌活性测试。结果表明,在质量浓度为200 mg/L时,目标化合物对东方黏虫具有中等杀虫活性,其中,5-溴-N-[(4-氯-2-甲基-6-甲酰基)苯基]-1-(3-氯-2-吡啶基)-3-硫甲基-1H-吡唑-4-甲酰胺杀虫活性为80%。在质量浓度为50mg/L时,部分化合物对5种病菌表现出中等的离体抑菌活性,N-[(4-氯-2-甲基-6-甲酰胺基)苯基]-1-(3-氯-2-吡啶基)-3-硫甲基-1H-吡唑-4-甲酰胺和N-[(4-氯-2-甲基-6-环丙基酰胺基)苯基]-1-(3-氯-2-吡啶基)-3-硫甲基-1H-吡唑-4-甲酰胺对番茄早疫病菌显示了良好的活性,分别为65.2%和67.1%,高于对照药百菌清。