6-Alpha-halopenicillanic acid 1,1-dioxides
US4420426A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Dec 9, 1980 |
| Grant date | Dec 13, 1983 |
| Priority date | — |
| Expiry date | Dec 9, 2000 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D499/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for the preparation of penicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo, which comprises oxidation of a 6-halopenicillanic acid, or an ester thereof readily hydrolyzable in vivo, to the corresponding 6-halopenicillanic acid 1,1-dioxide or ester thereof, followed by dehalogenation (e.g. by hydrogenolysis). Certain of the 6-halopenicillanic acid 1,1-dioxides and esters thereof readily hydrolyzable in vivo are novel intermediates. Penicillanic acid 1,1-dioxide, and esters thereof readily hydrolyzable in vivo are known compounds which are beta-lactamase inhibitors and which enhance the effectiveness of certain beta-lactam antibiotics (e.g. the penicillins) in the treatment of bacterial infections in mammals, particularly humans.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.