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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 B 1a . In this synthesis, thioglycosyl donors, but not trichloroacetimidates, were found compatible with sugar-macrolide synthesis under rt promotion with NIS or I 2 in N-methylpyrrolidone.
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