含螺噻唑烷酮的三氟乙基硫醚类化合物的合成与杀螨活性

    Synthesis and acaricidal activity of trifluoroethyl sulfide derivatives containing spirothiazolidinones

    • 摘要: 三氟乙基硫醚类杀螨剂因新颖的结构和良好的杀螨效果被研究。为寻找高杀螨活性化合物,以sulfiflumin为先导化合物,在其噻唑烷酮基团上引入螺环季酮酸类杀螨剂的螺环结构,设计并合成25个含螺噻唑烷酮的三氟乙基硫醚衍生物,采用核磁共振氢谱(1H NMR)、碳谱(13C NMR)和高分辨质谱(HRMS)对其结构进行表征。杀螨活性测试结果表明,在100 mg/L下,部分化合物对朱砂叶螨(Tetranychus cinnabarinus)和二斑叶螨(T. urticae)具有90%以上的杀螨活性,其中化合物VIIh对朱砂叶螨活性较高,半致死浓度(LC50)低至4.3 mg/L,稍高于sulfiflumin(1.1 mg/L)和乙唑螨腈(1.7 mg/L)。

       

      Abstract: Trifluoroethyl sulfide acaricides have been studied for their novel structures and excellent acaricidal efficacy. To discover new acaricides with high activities, 25 novel trifluoroethyl sulfide compounds containing spirothiazolidinones were designed and synthesized by introducing the spirocyclic fragment of spirocyclic tetronic acid acaricides to the thiazolidinone group based on the lead compound sulfiflumin. All the designed compounds were characterized by 1H NMR, 13C NMR and HRMS. Acaricidal activity tests showed that some of the designed compounds exhibited more than 90% activity against Tetranychus cinnabarinus and T. urticae at a dosage of 100 mg/L. Notably, compound VIIh was more effective against T. cinnabarinus with the LC50 value of 4.3 mg/L, which was slightly higher than sulfiflumin (1.1 mg/L) and cyetpyrafen (1.7 mg/L).

       

    /

    返回文章
    返回