三氟乙基硫醚（亚砜）类化合物TC-1和TC-2的设计、合成及杀螨活性

Design, synthesis and acaricidal activity of trifluoroethyl thioether (sulfoxide) derivatives TC-1 and TC-2

摘要:

为研发出高效的杀螨剂，以2-(氯甲基)-N-{2-氟-4-甲基-5-[(2, 2, 2-三氟乙基)硫代]苯基}苯甲酰胺(化合物Ⅶ)为先导化合物，经结构优化合成了2个三氟乙基硫醚（亚砜）类化合物TC-1和TC-2，并通过1HNMR、13CNMR和HRMS对化合物结构进行了表征。室内生物活性测试显示：当TC-1和TC-2质量浓度为10 mg/L时，TC-1和TC-2对朱砂叶螨（Tetranychus cinnabarinus）致死率分别为100%和90.6%。目标化合物表现出优异的杀螨活性，可作为进一步的先导化合物或候选杀螨剂品种进行深入研究与开发。

Abstract:

In order to discover and develop more efficient acaricides, two trifluoroethyl thioether (sulfoxide) derivatives TC-1 and TC-2 were synthesized by structural optimization with 2-(chloromethyl)-N-(2-fluoro-4-methyl-5-((2, 2, 2-trifluoroethyl)thio)phenyl)benzamide (compound Ⅶ) as lead compound. Their structures were confirmed by 1HNMR, 13CNMR and HRMS. Greenhouse acaricidal activity data showed that the mortality rates of TC-1 and TC-2 against Tetranychus cinnabarinus at 10 mg/L were 100% and 90.6%, respectively. Target compounds exhibited excellent acaricidal activity and can be used as lead compounds or candidate acaricides for further study and development.