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Synthesis of gem-difluoro-avermectin derivatives: potent anthelmintic and anticonvulsant agents
P T Meinke1, W L Shoop, B F Michael
1Merck Research Laboratories, Department of Medicinal Chemistry, Rahway, NJ 07065-0900, USA.
Bioorganic & Medicinal Chemistry Letters
|February 6, 1999
Abstract:
A series of gem-difluoro-avermectin derivatives was synthesized from the corresponding ketones at positions 4", 4', 13, and 23 using diethylaminosulfur trifluoride (DAST). These fluorinated avermectins exhibit potent antiparasitic activity in a new Haemonchus contortus larval assay and are equipotent to ivermectin. In addition, 23-gem-difluoro-ivermectin displays useful anticonvulsant activity in mouse models.