摘要
为发现高效杀虫剂,采用活性药效基团融合策略,以2-氟-3-氨基苯甲酸甲酯和2-三氟甲基苯胺为起始原料,设计合成了间二酰胺类化合物N-[2-溴-4-(全氟丙烷-2-基)-6-(三氟甲基)苯基]-3-[N-(氰甲基)苯甲酰胺基]-2-氟苯甲酰胺(NC-1),其结构经^(1)HNMR、^(13)CNMR和HRMS确证。初步的室内生物活性测试结果表明,化合物NC-1具有优异的杀虫活性,在质量浓度0.05 mg/L下对小菜蛾的致死率为96.67%,在质量浓度0.625 mg/L下对二化螟的致死率为93.33%。化合物NC-1可作为先导化合物或候选杀虫剂进行深入研究与开发。
In order to discover highly effective insecticide,a meta-dicaramide compound N-[2-bromo-4-(perfluoropropane-2-yl)-6-(trifluoromethyl)phenyl]-3-[N-(cyanomethyl)benzoylamino]-2-fluorobenzamide(NC-1)was designed and synthesized by an active pharmacophore fusion strategy using methyl3-amino-2-fluorobenzoate and 2-trifluoromethylaniline as starting materials.The structure of compound NC-1 was confirmed by ^(1)HNMR,^(13)CNMR and HRMS.The preliminary bioassay results in greenhouse showed that compound NC-1 exhibited excellent insecticidal activity.The mortality of compound NC-1against Plutella xylostella was 96.67%at mass concentration of 0.05 mg/L and that against Chilo suppressalis was 93.33%at mass concentration of 0.625 mg/L.Compound NC-1 could be used as a lead compound or a candidate insecticide for further research and development.
作者
张静
裴鸿艳
王锋
刘东东
高一星
张立新
ZHANG Jing;PEI Hongyan;WANG Feng;LIU Dongdong;GAO Yixing;ZHANG Lixin(School of Chemical Engineering,University of Science and Technology Liaoning,Anshan 114051,Liaoning,China;Institute of Functional Molecules,Shenyang University of Chemical Technology,Liaoning Province Key Laboratory of Green Functional Molecular Design and Development,Shenyang Key Laboratory of Targeted Pesticides,Shenyang 110142,Liaoning,China)
出处
《精细化工》
EI
CAS
CSCD
北大核心
2022年第4期769-774,共6页
Fine Chemicals
关键词
间二酰胺
杀虫活性
小菜蛾
二化螟
医药原料
meta-diamide
insecticidal activity
Plutella xylostella
Chilo suppressalis
drug materials
