间二酰胺类化合物NC-1的设计、合成及杀虫活性
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Design, synthesis and insecticidal activity of meta-diamide compound NC-1
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    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1HNMR、13CNMR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。

    Abstract:

    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 using the strategy of active pharmacophore fusion with methyl 2-fluoro-3-aminobenzoate and 2-trifluoromethylaniline as starting materials. The structure of compound NC-1 was confirmed by 1H NMR, 13C NMR and HRMS. The preliminary bioassay results in greenhouse showed that compound NC-1 exhibited excellent insecticidal activity, the mortality of compound NC-1 against Plutellaxylostella was 96.67 % at 0.05 mg/L and 93.33 % against Chilosuppressalis at 0.625 mg/L. Compound NC-1 can be used as a lead compound or a candidate insecticide for further research and development.

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张静,裴鸿艳,王锋,刘东东,高一星,张立新.间二酰胺类化合物NC-1的设计、合成及杀虫活性[J].精细化工,2022,39(4):0

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  • 收稿日期:2021-10-18
  • 最后修改日期:2021-11-25
  • 录用日期:2021-12-06
  • 在线发布日期: 2022-01-11
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