23-Keto derivatives of C-076 compounds
US4289760A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 2, 1980 |
| Grant date | Sep 15, 1981 |
| Priority date | — |
| Expiry date | May 2, 2000 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P33/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.