13-deoxy-23-oxo(keto) and 23-imino derivatives of 13-deoxy...

C - Chemistry – Metallurgy – 07 – D

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C07D 493/22 (2006.01) A01N 43/90 (2006.01) A01N 47/24 (2006.01) A01N 47/34 (2006.01) A23K 1/17 (2006.01) A61K 31/70 (2006.01) C07H 19/01 (2006.01)

Patent

CA 1301750

30,398-00 13-DEOXY-23-OXO (KETO) AND 23-IMINO DERIVATIVES OF 13-DEOXY C-076-AGLYCONE COMPOUNDS ABSTRACT OF THE INVENTION The present invention relates to novel 23-oxo (keto) and 23-imino derivatives of C-076 wherein the C-076 compounds are not substituted at the 13-position. The C-076 compounds (collectively) are isolates from the fermentation broth of Streptomyces avermitilis. The present 23-oxo compounds are prepared by selectively oxidizing suitably protected 13-deoxy C-076 aglycone compounds by using oxidizing agents. Subsequently, the 23-oxo compounds are converted to the 23-imino compounds. These novel compounds have potent anthelmintic, insecti- cidal, ectoparasiticidal, nematicidal and acaricidal activity. Compositions containing these 23-oxo and 23-imino derivatives of 13-deoxy C-076 aglycones also are described herein.

546552

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