Two series of milbemycin analogues containing ester and methoxy oxime groups were designed according to analog synthesis and sub-structure ligation from deglycosyl ivermectin, which is the analogue of milbemycin. The analogues reaction was carried out with the corresponding aromatic chloride, and the structures of the target compounds were confirmed by 1H NMR and high resolution mass spectra (HRMS). The insecticidal activities of 18 analogues against Tetranychus cinnabarinus, Mythimna sepatara and Aphis fabae were tested. The results showed that all analogues had different degree of insecticidal activity, especially compounds 4IIa and 4IIb showed the highest insecticidal activities against Mythimna sepatara and Aphis fabae.

Key words: milbemycin analogues, synthesis, biological activity