CEPHALOSPORINS AS INTERMEDIATE PRODUCTS IN SYNTHESIS OF CEPHALOSPORINS POSSESSING ANTIBACTERIAL PROPERTIES

摘要

NEW MATERIAL:A compound shown by the formulaI(R1 is H or carboxyl- protecting group; R2 is aromatic hydrocarbon group, acylamino, etc.; R3 is H or alkoxy; R4 is H or halogen; R5 is H or amino; A is -CH2-, etc.; Z is S,S O; one of dotted lines in the cephem ring is double bond) and its salt. EXAMPLE:7-[2-(2-Aminothiazole-4-yl)acetamido]-3-[2-(5-acetamido-1,2,3, 4-tetrazolyl) methyl]-DELTA3-cephem-4-carboxylic acid. USE:An antibacterial agent effective against Gram-positive and Gram-negative bacteria. Stable to beta-lactamse, having low toxicity. PROCESS:A compound shown by the formula II or its salt is reacted with an aromatic hydrocarbon, etc. in an organic solvent in the presence of an acid, etc., to give a compound shown by the formula III. This compound is reacted with a compound shown by the formula IV, to give shown by the formulaI.