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N-嘧啶三氟乙基硫醚/亚砜苯胺类化合物的设计、合成与杀螨活性

Design,synthesis and acaricidal activity of N-pyrimidine trifluoroethyl sulfide/sulfoxide aniline compounds
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摘要 [目的]研发高活性三氟乙基硫醚/亚砜类杀螨化合物。[方法]以sulfiflumin为先导化合物,引入杀虫(螨)剂中常见的嘧啶结构,设计并合成了15个N-嘧啶三氟乙基硫醚/亚砜苯胺类化合物,并对其进行杀螨活性测试。[结果]在100 mg/L质量浓度下,该系列化合物对朱砂叶螨和二斑叶螨均有一定的杀螨活性,且对二斑叶螨的活性远高于对朱砂叶螨的活性,大部分化合物对二斑叶螨的致死率高于90%。[结论]所合成化合物具有较好的杀螨活性,为三氟乙基硫醚/亚砜衍生物的设计和改造提供研究思路。 [Aims]This study aims to generate trifluoroethyl sulfide/sulfoxide compounds with excellent acaricidal activity.[Methods]The lead compound sulfiflumin was modified by introducing the pyrimidine structure commonly found in insecticides/acaricides.Fifteen N-pyrimidine trifluoroethyl sulfide/sulfoxide aniline compounds were designed and synthesized,and their acaricidal activities were tested.[Results]The synthesized compounds had certain acaricidal activity against Tetranychus urticae and T.cinnabarinus at the dosage of 100 mg/L.The activity against T.urticae is much higher than that of T.cinnabarinus and the mortality of most compounds against T.urticae was higher than 90%.[Conclusions]The synthesized compounds with good acaricidal activity provide a guideline for the design of trifluoroethyl sulfide/sulfoxide compounds.
作者 王佳鑫 蔡胜梅 田平义 包如胜 刘祈星 周海峰 WANG Jiaxin;CAI Shengmei;TIAN Pingyi;BAO Rusheng;LIU Qixing;ZHOU Haifeng(Research Center of Green Pharmaceutical Technology and Process,Hubei Key Laboratory of Natural Products Research and Development,College of Biological and Pharmaceutical Sciences,China Three Gorges University,Yichang 443002,Hubei,China;Hangzhou Electrochemical Group Auxiliary Chemical Co.,Ltd.,Hangzhou 311228,China;Taizhou Key Laboratory of Green Agrochemicals Development,Synwill Co.,Ltd.,Taizhou 318000,Zhejiang,China)
出处 《农药》 北大核心 2025年第12期868-875,共8页 Agrochemicals
基金 顺毅股份有限公司研发项目(SDHZ2021215) 国家自然科学基金(22278244)。
关键词 三氟乙基硫醚/亚砜 嘧啶 杀螨活性 合成 trifluoroethyl sulfide/sulfoxide pyrimidine acaricidal activity synthesis
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