New potent insecticidal agent: 4′-fucosyl avermectin derivative

A 4′-fucosyl avermectin derivative was designed and synthesized. This new avermectin derivative showed excellent in vivo bioactivity against cabbage larvae when compared to commercially available avermectin B1a. In this synthesis, thioglycosyl donors, but not trichloroacetimidates, were found compatible with sugar-macrolide synthesis under rt promotion with NIS or I2 in N-methylpyrrolidone.