新型间二酰胺类杀虫剂的设计、合成及生物活性

Design,Synthesis and Biological Activity of Novel Meta-diamide Insecticides

为了开发出高活性、低成本的杀虫剂,以溴虫氟苯双酰胺先导化合物,通过活性亚结构拼接法合成出6个间二酰胺类化合物,并经过^(1)H NMR、^(13)C NMR和HRMS等表征手段对目标化合物Ⅰa~Ⅰf的结构进行了确认。室内杀虫、杀螨活性测试结果显示,Ⅰa~Ⅰf对小菜蛾3龄幼虫和二斑叶螨成螨均有不错的活性。对小菜蛾幼虫,Ⅰa和Ⅰe具有最好的活性,在100 mg/L时Ⅰa和Ⅰe都具有100%的杀虫活性,在50 mg/L时Ⅰa和Ⅰe的活性分别是93%,72%。对二斑叶螨成螨,Ⅰa和Ⅰd具有最好的活性,在100 mg/L时Ⅰa和Ⅰd都具有100%的活性,在50 mg/L时Ⅰa和Ⅰd的活性分别是92%,87%。

In order to develop insecticides with high activity and low cost,six meta-diamides were synthesized by active substructural splicing method with Broflanilide as the lead compound,and the structure of the target compound Ⅰa~Ⅰf was confirmed by ^(1)H NMR,^(13)C NMR and HRMS.The results of indoor insecticidal and acaricidal activity tests showed that Ⅰa~Ⅰf had good activity against the 3rd instar larvae of Plutella xylostella and adult mites of Tetranychus urticae.For diamondback moth larvae,Ⅰa and Ⅰe have the best insecticidal activity.At 100 mg/L,Ia and Ie have 100% insecticidal activity,and at 50 mg/L,Ⅰa and Ⅰe have 93% and 72% insecticidal activity,respectively.For adults of Tetranychus urticae,Ⅰa and Ⅰd have the best activity.At 100 mg/L,Ia and Id have 100% activity,and at 50 mg/L,Ⅰa and Ⅰd have 92%and 87%activity,respectively.