| 摘要 |
1287786 Cephalosporanic acid derivatives CIBA-GEIGY AG 3 Nov 1969 [7 Nov 1968 26 April 1969] 53698/69 Heading C2A O-Desacetyl-7-N-acyl-amino-cephalosporanic acids of the Formula I in which R 1 represents an acetyl residue which contains a cyclopentyl, cyclohexyl, phenyl, pyridyl, thienyl or furyl residue, said residues being unsubstituted or substituted by one or more C 1-5 alkyl, hydroxyl, C 1-5 alkoxy, trifluoromethyl, or nitro groups or halogen atoms and which acetyl residue contains a free amino group in α-position to the carbonyl group, R 2 stands for C 1-5 alkyl which is unsubstituted or substituted by one or more halogen atoms, and n is 0 or 1, and their salts (including inner salts) are prepared from a compound of the Formula II by introducing the acyl residue R 1 into the 7- amino group; or from compounds of Formula I in which the free amino group in R 1 and/or the 4-carboxyl group is/are protected, the protective group(s) being split off, and, if desired, a result ing free compound is converted into a salt or a resulting salt into the free compound or into another salt, and/or, if desired, a resulting mixture of isomers is resolved into the individual isomers. Salts referred to include alkali metal (e.g. Na or K), alkaline earth metal (e.g. Mg or Ca), ammonium, trialkylamine, 1-methyl-pyrrolidine, 1-ethyl-piperidine, dibenzyl-ethylenediamine and procaine salts; and acid addition salts with hydrochloric, hydrobromic, sulphuric, methanesulphonic, 2-hydroxyethanesulphonic, p-toluenesulphonic and trifluoroacetic acid. The starting materials of Formulµ I and II are prepared by a variety of known methods. Antibacterial compositions having activity against gram-negative and gram-positive bacteria comprise the above O-desacetyl-7-N-acyl amino-cephalosporanic acids or a salt thereof in admixture or conjunction with a pharmaceutically suitable carrier. The compositions may be administered enterally, parenterally or topically in the form of tablets, dragees, capsules, suppositories, solutions, suspensions, emulsions, ointments or creams. |
