Synthesis of new, potent avermectin-like insecticidal agents

摘要

4'-Modified avermectin derivatives were designed and synthesized. Some of the new synthetic compounds showed excellent in vivo bioactivity against cabbage larvae when compared to commercially available avermectin B-1a. In this synthesis, uncommon thioglycosyl sugar donors, prepared from the hydrolysis of natural antibiotics, proved compatible with sugar-macrolide synthesis in the presence of N-iodosuccinimide (NIS) or I-2 in N-methylpyrrolidone at room temperature. (c) 2005 Published by Elsevier Ltd.