Nagai K et al. (2003) Bioorg Med Chem Lett "Synthesis and biological activities of novel 4"-alkylidene avermectin derivatives."

Harder A, Turberg A, Sunazuka T, Omura S, Nagai K, Shiomi K

[Bioorg Med Chem Lett, 2003]

Horner-Emmons reaction of 4"-dehydro-5-O-TBDMS-avermectin B-1a with a variety of phosphorus ylides using LHMDS gave novel 4"-alkylidene avermectin derivatives in high yields. Further modifications led to derivatives bearing diverse functional groups. The new avermectin derivatives showed potent growth inhibitory activity against Artemia salina and Caenorhabditis elegans.