摘要/Abstract

为了发现结构新颖的高效杀虫剂，利用活性亚结构拼接的方法，设计并合成了11个未见文献报道的新型含环丙基的间二酰胺类化合物，其结构经过¹H NMR，¹³C NMR和HRMS确证.初步的生物活性测试结果表明，部分化合物对小菜蛾和二化螟表现出了较好的杀虫活性.其中N-（2-溴-4-（全氟丙烷-2-基）-6-（三氟甲基）苯基）-3-（N-（环丙基甲基）苯甲酰胺基）-2-氟苯甲酰胺（6d）和3-（N-（环丙基甲基）苯甲酰胺基）-N-（2，6-二溴-4-（全氟丙烷-2-基）苯基）-2-氟苯甲酰胺（6e）在1 mg/L测试浓度下对小菜蛾的杀虫活性都为100%，化合物6d在5 mg/L测试浓度下对二化螟的杀虫活性为100%.
关键词: 合成, 环丙基, 间二酰胺, 杀虫活性
To discover novel insecticide with improved activity, a series of meta-diamide compounds containing cyclopropyl moiety were synthesized on the principle of biologically active factor splicing. The structures of synthetic derivatives were characterized by ¹H NMR, ¹³C NMR and HRMS. Preliminary bioassay data showed that some of the title compounds exhibited good insecticidal activities against Plutella xylostella and Chilo suppressalis. Among them, the mortality of N-(2-bromo-4-(perfluoropropan-2-yl)-6-(trifluoromethyl)phenyl)-3-(N-(cyclopropylmethyl)benzamido)-2-fluorobenzamide (6d) and 3-(N-(cyclopropylmethyl)benzamido)-N-(2,6-dibromo-4-(perfluoropropan-2-yl)phenyl)-2-fluorobenzamide (6e) was 100% against Plute-lla xylostella at 1 mg/L, and the mortality of compound 6d was 100% against Chilo suppressalis at 5 mg/L.
Key words: synthesis, cyclopropyl, meta-diamide, inseticidal activity


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