- 6-beta-Halopenicillanic acid 1,1-dioxides as beta-lactamase inhibitors
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6-beta-Halopenicillanic acid 1,1-dioxides, physiologically acceptable salts thereof and esters thereof readily hydrolyzable; pharmaceutical compositions containing a 6-beta-halopenicillanic acid 1,1-dioxide, a physiologically acceptable salt thereof or an ester thereof readily hydrolyzable; and a method for enhancing the effectiveness of a beta-lactam antibiotic, using a 6-beta-halopenicillanic acid 1,1-dioxide, a physiologically acceptable salt thereof or an ester thereof readily hydrolyzable.
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- ACETOXYMETHYL PENAM COMPOUNDS AS BETA-LACTAMASE INHIBITORS
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2-beta-Acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxide, pharmaceutically-acceptable salts thereof and esters thereof readily hydrolyzable in vivo; pharmaceutical compositions containing 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxide or salt or ester thereof; and method of enhancing the effectiveness of a beta-lactam antibiotic using 2-beta-acetoxymethyl-2-alpha-methyl-(5R)penam-3-alpha-carboxylic acid 1,1-dioxide or salt or ester thereof
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- DERIVATIVES OF 6BETA-HYDROXYALKYLPENICILLANIC ACIDS AS BETA-LACTAMASE INHIBITORS
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6beta-Hydroxyalkylpenicillanic acids and derivatives thereof as useful enhancers of the effectiveness of several beta-lactam antibiotics against many beta-lactamase producing bacteria, and 6beta-substituted penicillanic acid benzyl ester derivatives as useful intermediates leading to said agents which enhance the effectiveness of beta-lactam antibiotics
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- Penam 1,1-dioxides as beta-lactamase inhibitors
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(3S, 5R)-Penam-3-carboxylic acid 1,1-dioxide, optionally having a methyl group at the 2-position, and esters thereof readily hydrolyzable in vivo, are useful for enhancing the effectiveness of several beta-lactam antibiotics against many beta-lactamase producing bacteria.
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- Process for preparing cephalosporines
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A process for preparing cephalosporines in which a cephalosporanic derivative is treated with a polar solvent, then with an organic base to give a mixture which is cooled at a temperature lower than -25° C. A cyclic derivative of boron is added to the mixture and the temperature is increased to about 0° C. An intermediate compound is formed which by treatment first with an acylating agent and then with a mixture of water and alcohol provides a solution containing cephalosporines.
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- 7-[5-N-(n-Butoxyethoxy carbonyl and 2-chloroethoxy carbonyl)-amino] cephalosporins C
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New and useful cephem compounds derived from cephalosporin C are provided by this invention, which are valuable as intermediate for the synthesis of another bacteriocidally active cephem derivatives and which are readily extractable from its aqueous solution by means of an organic solvent and enable the cephalosporin C content in the aqueous fermentation broth filtrate to be recovered at an improved yield. Cephalosporin C present in the fermentation broth may be converted into the cephem compounds of this invention by reacting with a substituted chloroformate compound within said filtrate, and the cephem compounds so formed may then be extracted therefrom with an organic solvent. The cephem compounds of this invention further may be converted into a 7-acylamidocephalosporanic acid or 7-aminocephalosporanic acid through some successive reactions.
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