NOVEL CEPHALOSPORANIC ACID DERIVATIVE* ITS OPTICAL ISOMER* ITS NONTOXIC SALT* AND THEIR PREPARATION

摘要

NEW MATERIAL:A compound of formula I: [R<1> is H, acetoxyl, pyridinium group, etc,; Z is COOR<2> (R<2> is H, alkali metal, alkylammonium, etc.), or COOR<-> when R<1> is pyridinium group; Y is NO2, OH, protected OH group, etc.], its optically active substance or nontoxic salt. EXAMPLE:Sodium 7-(P-hydroxytropoylamido)-3-acetoxymethyl-3-cephem-4-carboxylate. USE:Antibacterials and intermediates for their synthesis. Effective against Gram- positive and Gram-negative vacterial. PROCESS:A 7-aminocephalosporanic acid derivative of formula II is reacted with a tropic acid derivative or its reactive derivative of formula III: (R<3> is H or alcohol- protecting group) in a solvent, e.g. acetone, and, if necessary, the protecting group is removed to give the compound of formula I.