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Paper | Regular issue | Vol 104, No. 3, 2022, pp.512-523
Published online, 17th December, 2021
DOI: 10.3987/COM-21-14593
Design, Synthesis and Insecticidal Activity of 3-Arylisoxazoline-N-alkylpyrazole-5-carboxamide Derivatives against Tetranychus urticae Koch

Shuhao Qu,* Lifei Zhu, Qiang Wang, and Xiaoli Wang

*School of Veterinary Medicine, Henan University of Animal Husbandry and Economy, Zhengzhou 450046, China.


Starting from ethyl 5,5-dimethoxy-2,4-dioxopentanoate 2, 3-arylisoxazoline-N-alkylpyrazole-5-carboxamide derivatives 1a-1d were designed and synthesized with the key steps of 1,3-dipolar cycloaddition and EDCl coupling. Their insecticidal activity against Tetranychus urticae Koch was further evaluated and the results indicated that, compared with Fluralaner, all 1a-1d showed moderate and less activity at 500 mg/L and 250 mg/L, respectively. This study complements the structure-activity relationship of N-alkylpyrazole-5-carboxamides to Fluralaner, giving further guidance in Fluralaner-based pesticide drug design and discovery.