Synthesis and insecticidal activity of novel 1,2,4-triazole derivatives containing trifluoroacetyl moieties

A series of compounds containing trifluoroacetyl groups were synthesized, and their insecticidal activity against Nilaparvata lugens and Aphis craccivora was evaluated. The compound structure was identified by NMR, HRMS, and single-crystal diffraction. The bioassay results indicated that compound 4-1 (R¹ is chloropyridine, R² is H), 4-2 (R¹ is chlorothiazole, R² is H) and 4-19 (R¹ is benzyl, R² is isopropyl) had the best activity against Nilaparvata lugens (93.5%, 94.1% and 95.5%) at 100 mg/L concentration. The effect of different substituents of R¹ or R² on the activity was studied through the structure-activity relationship. Molecular docking of compounds 4-1 and 4-2 was discussed.