3-Carbamyloxymethyl-cephalosporins
AssigneeEli Lilly and Company
InventorRamakrishnan Nagarajan
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Abstract
The present invention is directed to 7-amino-3-carbamoyloxymethyl-3-cephem-4-carboxylic acid: ##STR1## and to precursors and derivatives. The compound, its precursors, and its derivatives exhibit antibacterial activity, which, in the instance of certain of the derivatives, is of an enhanced degree.
Claims5
The compound of the formula ##STR28## wherein R.sup.o represents hydrogen or R.sup.1, and R.sup.1 represents alkyl of C.sub.1 -C.sub.6, 2,2,2-trichloroethyl, 2-iodoethyl, tert-alkenyl of C.sub.5 -C.sub.7, tert-alkynyl of C.sub.5 -C.sub.7, benzyl, nitrobenzyl, tetrahydropyranyl, succinimidomethyl, phthalimidomethyl, methoxybenzyl, dimethoxybenzyl, cyanomethyl, nitrophenyl, dinitrophenyl, 2,4,6-trinitrophenyl, bis(p-methoxyphenyl)methyl, triphenylmethyl, diphenylmethyl, benzyloxymethyl, loweralkanoyloxymethyl of C.sub.3 -C.sub.6, loweralkanoyl of C.sub.2 -C.sub.4, phenacyl, or radical of the formula ##STR29## wherein each R.sup.2 independently represents loweralkyl of C.sub.1 -C.sub.4 or halo selected from the group consisting of bromo, chloro, fluoro, and iodo, subject to the limitation that at least one R.sup.2 represents loweralkyl as defined;
- and R.sup.3 represents amino or an acylamido group where the acyl group is:
- alkanoyl of C.sub.1 -C.sub.4,
- aroyl of C.sub.6 -C.sub.12,
- alkoxycarbonyl of C.sub.1 -C.sub.4,
- benzyloxycarbonyl,
- cycloalkoxycarbonyl of C.sub.5 -C.sub.6,
- aryloxycarbonyl of C.sub.6 -C.sub.12,
- one of the above groups substituted with from one to three groups, each selected from the group consisting of halo, nitro, loweralkoxy of C.sub.1 -C.sub.4, cyano, and, in the instance of aroyl and aryloxy, by loweralkyl of C.sub.1 -C.sub.4, or phthaloyl, subject to the limitation that at least one of the following exists:
- (1) R.sup.o represents R.sup.1 ;
- or (2) R.sup.3 represents acylamido as defined.
Dependencies are inferred from the claim text.