Avermectin degradation products and derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 493/22 (2006.01) A01N 43/90 (2006.01) A01N 55/00 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01) C07H 23/00 (2006.01)

Patent

CA 2052860

31/DLR30 18107 TITLE OF THE INVENTION AVERMECTIN DEGRADATION PRODUCTS AND DERIVATIVES ABSTRACT OF THE DISCLOSURE Novel avermectin derivatives are disclosed, wherein the C-17-21-25-dioxaspirane substructure has been disassembled and modified to include oxygen substitution at C-24 and C-25 and examples of C-24 and C-25 substituents are hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl groups. These compounds can be further substituted at the 4"-, 5-, 13-, and 23- positions. The new C-24 and C-25 substituted avermectin derivatives are prepared by cleavage of known and suitably protected avermectin compounds. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

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