23-Keto derivatives of C-076 compounds

Details 23-Keto derivatives of C-076 compounds 23-Keto derivatives of C-076 compounds

1980-05-02

1981-09-15

Jiles, Henry

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

424279, 536 17A, 26034341, 435119, A61K 3171, A61K 31335, C07H 1708, C07D31300

Patent

active

042897602

ABSTRACT:
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.

REFERENCES:
patent: 4156720 (1979-05-01), Fisher et al.
patent: 4171314 (1979-10-01), Chabala et al.
patent: 4172940 (1979-10-01), Chaiet
patent: 4199569 (1980-04-01), Chabala et al.
patent: 4200581 (1980-04-01), Fisher et al.
patent: 4201861 (1980-05-01), Mrozik et al.
patent: 4203976 (1980-05-01), Fisher et al.
patent: 4206205 (1980-06-01), Mrozik et al.

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