In searching for novel insecticide lead, 21 new meta-diamide compounds containing sulfide, sulfoxide and sulfone were designed and synthesized regarding Cyproflanilide as leading compound. All the compounds were characterized by ¹H NMR, ¹³C NMR and HRMS. The preliminary bioassay indicated that most of the title compounds exhibited excellent insecticidal activities against Nilaparvate lugens. Especially, the compound: N-(3-((2-bromo-6-(ethylthio)-4-(perfluoropropan-2-yl)phe-nyl)carbamoyl)-2-fluorophenyl)-N-(cyclopropylmethyl)nicotinamide (9d), exhibited 98.92 % mortality against N. lugens at 100 mg/L, better than cyproflanilide (0.00 % at 400 mg/L). Preliminary structure–activity relationship was also discussed based on insecticidal tests. This work helps in further exploitation of meta-diamide insecticide against hemipteran pests.

在寻找新型杀虫剂先导的过程中，以环丙苯胺为先导化合物，设计合成了21个含硫化物、亚砜和砜的间二酰胺类化合物。所有化合物均通过¹ H NMR、¹³ C NMR 和 HRMS 进行了表征。初步生物测定表明，大多数标题化合物对褐飞虱表现出优异的杀虫活性。特别地，化合物：N- (3-((2-溴-6-(乙硫基)-4-(全氟丙-2-基)苯基)氨基甲酰基)-2-氟苯基)-N-(环丙基甲基)烟酰胺( 9d ), 对褐飞虱表现出 98.92% 的死亡率在 100 mg/L 时，优于环丙苯胺（在 400 mg/L 时为 0.00%）。还根据杀虫试验讨论了初步的构效关系。这项工作有助于进一步开发间位二胺杀虫剂来对抗半翅目害虫。