Synthesis analogues of milbemycin and their bioactivity evaluation

Eight new 13-O-aminocarbonylivermectin aglycones and 4′-O-aminocarbonylivermectin monosaccharide were synthesized from ivermectin aglycone and ivermectin monosaccharide by the selective protection of C5-OH group. Their bioactivities were evaluated against spider mites (Tetranychus cinnabarinus), aphid (Aphis fabae) and orlental armyworm (Mythimma sepatara). Their structures were confirmed by 1H NMR, MS.