Carboxymethyl alkene amide Joseph Aros porin

摘要

NEW MATERIAL:The 7beta-carboxyalkenoylamino-3-cephem-4-carboxylic acid of formula I (R is aryl or heterocyclic group; R1 is H or halogen; R2 is single bond, O, etc.; R3 is single bond or alkylene; R4 is H or methoxy; R5 is H or 3-substitution group of cephalosporins; X is O, S, etc.). EXAMPLE:7-[2-( 2-Benzyloxycarbonylamino-4-thiazolyl)-3-benzyloxycarbonylmethylacrylam ino]-3-pyridinium methyl-3-cephem-4-carboxylate. USE:An antibacterial agent and a material for the testing of the sensitivity to bacteria. Effective especially to Gram-negative bacteria. PREPARATION:The objective compound can be prepared by the amidation of the carboxylic acid of formula III with the amine of formula II in a solvent in the presence of a condensation agent such as N,N'-diethylcarbodiimide, etc. preferably at -20-+50 deg.C for 10min-10hr.