新型七氟异丙基取代2,2-二氟-1,3-苯并二氧-5-乙酰胺衍生物的合成与杀虫活性

Synthesis and insecticidal activity of novel heptafluoroisopropyl substituted 2,2-difluoro-1,3-benzodioxol-5-acetamide derivatives

摘要: 为探索环境友好新型农药先导化合物，通过水相中酰胺缩合反应合成了16个未见文献报道的七氟异丙基苯基取代的2,2-二氟-1,3-苯并二氧-5-乙酰胺类目标化合物。其结构通过核磁共振氢谱、氟谱以及高分辨质谱确认。初步生物活性测定表明，部分目标化合物对蚕豆蚜虫和粘虫表现出良好的杀虫活性，初步构效关系显示苯环上取代基的种类和位置在化合物的杀虫活性中起关键作用。

Abstract: In order to discover novel and environmentally benign pesticides, a series of novel heptafluoroisopropyl substituted 2,2-difluoro-1,3-benzodioxol-5-acetamide derivatives were synthesized via amide condensation reaction in aqueous solution. All the title compouds were characterized by ¹H NMR, ¹⁹F NMR and HRMS. The bioassays showed that some of the compounds exhibited good insecticidal activities against bean aphids (Aphis craccivora) and armyworms (Mythimna separata). Preliminary structure-activity relationship studies suggested that the substituent groups played a key role in the insecticidal activities of the compounds.