23-keto derivatives of c-076 compounds

Details 23-keto derivatives of c-076 compounds 23-keto derivatives of c-076 compounds

C - Chemistry, Metallurgy

07

H

195/87, 260/230.

C07H 17/08 (2006.01) A01N 43/90 (2006.01) C07D 313/00 (2006.01) C07H 19/01 (2006.01) C12P 19/62 (2006.01)

Patent

CA 1168605

ABSTRACT OF THE DISCLOSURE Derivatives of C-076 compounds are described in which the C-076 molecule, a series of macrolides, has the 23-hydroxy group thereof oxidized to the 23-keto group. The 23-keto compounds are prepared by selectively oxidizing the suitably protected 23- hydroxy compound using such oxidizing agents as pyridinium dichromate, chromic acid-dimethyl pyrazole, chromic acid, chromic acid-acetic acid, and the like. Alternatively, selective oxidation of the unprotected 23-hydroxy compound may be accomplished by placing the compound in soil. Further reaction of the oxidized C-076 compounds is also possible. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal, and acaricidal activity. Compositions containing the described C-076 derivatives as the active ingredient thereof are also disclosed.

376580

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