嘧虫胺的合成及生物活性

Synthesis and Insecticidal Activity of Flufenerim

[目的]嘧虫胺(flufenerim)是由日本宇部兴产公司发现的一个新型嘧啶类杀虫剂,现由住友化学开发。为了研究其活性,对其合成方法进行了探索并进行了生物活性测试。[方法]以丙酰乙酸乙酯、磺酰氯、4-三氟甲氧基苄溴、氰化钠为起始原料制备了嘧虫胺。[结果]反应总收率40%,其结构经核磁验证。[结论]生测结果表明该化合物在低剂量下对小菜蛾和桃蚜具有较好的杀虫活性,对黏虫和朱砂叶螨也具有一定的活性。

[Aims] Flufenerim as a novel pesticide was discovered by UBE and developed by Sumitomo Chemical Co., Ltd. In order to study the insecticidal activity of flufenerim, the synthetic method and insecticidal bioassays were explored. [Methods] Flufenerim was synthesized by using ethyl 3-oxopentanoate, sulfonyl chloride, 1-（bromomethyl）-4- （trifluoromethoxy）benzene and sodium cyanide as start materials. [Results] The overall yield of flufenerim was 40% and its structure was confirmed by ^1H NMR. [Conclusions] The test results of biological activity showed that flufenerim exhibited good insecticidal activity against diamondback moths and green peach aphid at very low doses, and some activity to arrnywormand carmine spider mite as well.