Avermectin derivatives

Details Avermectin derivatives Avermectin derivatives

C - Chemistry, Metallurgy

07

H

167/202, 260/227

C07H 17/08 (2006.01) A01N 43/90 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01)

Patent

CA 2009824

8045/DLR11 17860 TITLE OF THE INVENTION AVERMECTIN DERIVATIVES ABSTRACT OF THE DISCLOSURE There are disclosed novel avermectin derivatives wherein the 3"- or 3'-methoxy group and/or the 4"- or 4'-hydroxyl group are replaced by hydrogen. The 3"- or 3'-desmethoxy-avermectins can further be derivatized at the 4"- or 4'-posîtions as the amino, semicarbazone or oxime analogs. The 3"- or 3'-desmethoxy-avermectins are prepared by the reaction of Samarium iodide on the corresponding 4"- or 4'-oxo-avermectins. The 4"-or 4'-deoxo- avermectins are prepared by radical deoxygenation of the corresponding hydroxy-avermectins. Di-de- oxygenated avermectin derivatives are obtained by combination of these two methods or by treating avermectin aglycone or avermectln monosaccharide with a dihydropyran. The new eompounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

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