新型杀虫剂Isocycloseram的合成与杀虫活性

The Synthesis and Insecticidal Activity of Isocycloseram

[目的]Isocycloseram是由瑞士先正达公司开发的新型异唑啉类杀虫剂,探索了其合成方法,并测试其杀虫活性。[方法]以4-溴-2-甲基苯甲酸和D-环丝氨酸为起始原料经9步反应成功制备isocycloseram,并经核磁及高分辨质谱表征验证其结构。[结果]所述合成路线反应收率较高。室内杀虫测试结果表明:isocycloseram对鳞翅目害虫小菜蛾、黏虫和二化螟及蜱螨目害虫朱砂叶螨具有较高的杀虫活性。

[Aims] Isocycloseram is a novel isoxazoline insecticide developed by Syngenta. The synthetic method for isocycloseram was explored, and its insecticidal activities were tested. [Methods] Isocycloseram was synthesized successfully with 4-bromo-2-methylbenzoic acid and D-cycloserine as starting materials by 9 steps. Meanwhile, the structural characterization of isocycloseram was identified by 1H NMR and H RMS. [Results] Isocycloseram was afforded in a medium yield by the synthetic method presented in this paper. The insecticidal assays indicated that isocycloseram exhibited excellent insecticidal activities against Lepidoptera pests(e.g. Plutella xylostella, Mythimna separate and Chilo suppressalis) and Acarina(e.g. Tetranychus cinnabarinus).