| 摘要 |
<p>A process for the preparation of penicillanic acid 1,1-dioxide and esters thereof readily hydrolyzable in vivo. Said process involves oxidation of a 6-halo derivative of penicillanic acid, or an ester thereof readily hydrolyzable in vivo, to the corresponding 6-halo derivative of penicillanic acid 1,1-dioxide or ester thereof, followed by dehalogenation (e.g. by hydrogenolysis). The 6-halo derivatives of penicillanic 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 useful as beta-lactamase inhibitors and for enhancing the effectiveness of certain beta-lactam antibiotics (e.g. the penicillins) in the treatment of bacterial infections in mammals, particularly humans.</p> |
