To discover novel, highly active, and eco-friendly insecticides, 20 unreported diamide compounds were designed via active substructure splicing strategy using cyproflanilide as the lead. Their structures were confirmed by 1H NMR, 13C NMR, and HRMS. Preliminary bioassays showed that although the target compounds did not significantly improve activity against lepidopteran pests including Plutella xylostella and Mythimna separata, progress was made against hemipteran pests. Some compounds exhibited good activity against Aphis craccivora and Nilaparvata lugens. Notably, compound N-(3-((2-bromo-6-(difluoromethoxy)-4-(perfluoropropan-2-yl)phenyl)carbamoyl)-2-fluorophenyl)-N-(1,1-dioxidotetrahydrothiophen-3-yl)-6-(trifluoromethyl)nicotinamide(8e) showed outstanding efficacy, with 100.0% insecticidal activity against Aphis craccivora at 10 mg/L and 97.6% against Nilaparvata lugens at 40 mg/L, significantly outperforming the control cyproflanilide. This study provides lead candidates for developing novel diamide insecticides and offers new solutions for managing hemipteran pests.
Xia Jiaoyun
,
Liu Chang
,
Hu Letian
,
Xiang Juncheng
,
Lv Liang
,
Pang huailin
,
Liu Jiyong
. Design, Synthesis, and Biological Activity Study of Novel Tetrahydrothiophene-Substituted Diamidesle[J]. Chinese Journal of Organic Chemistry, 0
: 3012
.
DOI: 10.6023/cjoc202603012
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