3-(5-三氟乙硫基)苯基-2,3-二氢喹唑啉-4(1H)-酮类衍生物的设计、合成及杀螨活性

Design, Synthesis and Acaricidal Activity of 3-(5-Trifluoroethylsulfanyl-phen-1-yl)-2,3-dihydroquinazolin-4(1H)-one Derivatives

[目的]发现高活性的杀螨化合物。[方法]采用骨架跃迁的策略,设计、合成了10个3-(5-三氟乙硫基)苯基-2,3-二氢喹唑啉-4(1H)-酮类新化合物,其结构经1H NMR确证,并进行杀朱砂叶螨的活性测试。[结果]生物活性数据表明,化合物7a、7b、7c、9a、9b在100 mg/L剂量下,对朱砂叶螨致死率达100%,其中化合物7b和9b在5 mg/L剂量下,对朱砂叶螨的致死率分别为97.3%和86.0%。[结论]目标化合物7b、7c、9b,在100、10 mg/L剂量下对朱砂叶螨具有令人满意的活性,其中7b和9b在5 mg/L更低剂量下对朱砂叶螨仍表现出优异的杀螨活性,值得深入研究。

[Aims] The aims were to discover new acaricidal compounds with high activity. [Methods] Ten novel3-（ 5-trifluoroethylsulfanyl-phen-1-yl）-2, 3-dihydroquinazolin-4（ 1 H）-one compounds were designed and prepared utilizing skeleton hopping strategy, and their structures were characterized by1 H NMR. Their acaricidal activities against Tetranychus cinnabarinus were tested. [Results] Biological activities of the target compounds showed that the mortality rates of compounds 7 a, 7 b, 7 c, 9 a and 9 b against T. cinnabarinus at 100 mg/L were all 100%. Among them,the mortality rates of 7 b and 9 b at 5 mg/L were 97.3 and 86.0%, respectively. [Conclusions] The target compounds 7 b,7 c and 9 b possessed satisfied acaricidal activities at 100 and 10 mg/L, especially compounds 7 b and 9 b exhibited excellent acaricidal activities even at lower concentration of 5 mg/L, which are worth further study.