CEPHEM DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF

摘要

Cephem derivatives of the formula wherein (i) Z is 1,4-dihydro-4-oxo-1-pyridyl or the corresponding group substituted by at least one of alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, OH, F, Cl, Br, I, NO2 or NH2 and R is -S-Het wherein Het is 3-methyl-1,2,4-thiadiazolyl-5, 5-methyl-1,3,4-oxadiazolyl-2, 5-hydroxymethyl-1,3,4-oxadiazolyl-2, 5methyl-1,3,4-thiadiazolyl-2, 5-hydroxy-methyl-1,3,4-thiadiazolyl-2,tetrazolyl-5,1-methyltetrazolyl-5, 1,2,3-triazolyl-4, 4-methyl-oxazolyl-2 or 1-oxidopyridinio-2, or (ii) Z is 3,5-dichloro-1,4-dihydro-4-oxo-1-pyridyl and R is -OCOCH3 and esters thereof which are readily split, and the physiologically acceptable salts thereof, possess anti-bacterial activity. They can be prepared by reacting a 3-CH2R-7-amino-3-cephem-4-carboxylic acid or a functional derivative thereof with a pyridone acetic acid of the formula Z-CH2-COOH or a functional derivative thereof; or by reacting a 3-CH2R-7-(X-acetamido)-3-cephem-4-carboxylic acid wherein X is Cl, Br or a reactively esterified OH-group, or a functional derivative thereof, with a pyridone of the formula Z-H wherein Z has the values given above, or a functional derivative thereof; or by liberating a functionally modified OH-, HN2- or oxo-group present in a compound otherwise corresponding to a product of the above formula by treatment with a solvolyzing or hydrogenolyzing agent.