Nine rotenone oxime ester derivatives were synthesized from natural rotenone with two steps. Their structures were clearly established by ¹H NMR, IR spectra and elemental analysis. The pre-liminary bioassays indicated that compounds 3a, 3b and 3c exhibited 80.0%, 90.0% and 95.0% mortality against Musca domestica at 0.30 mg/mL and 57.1%, 60.0% and 73.3% mortality against Spodoptera exigua at 0.10 mg/mL, respectively. 3b exhibited 86.4% mortality against Mythimna separata at 1.00 mg/mL and 71.8% mortality against Nephotettix cincticeps at 0.50 mg/mL. 3c exhibited 100% mortality against Mythimna separata at 1.00 mg/mL. 3a exhibited 54.2% mortality against Nephotettix cincticeps at 0.50 mg/mL.

Key words: rotenone oxime ester, synthesis, biological activity