Verfahren zur Herstellung neuer Derivate der 7-Aminocephalosporansäure

摘要

1325889 Cephalosporanic acids CIBA-GEIGY AG 28 Sept 1970 [10 Oct 1969] 46038/70 Heading C2A Novel cephalosporanic acids of Formula I wherein R 1 is an aminopyridinium group which may be substituted and R 2 is hydrogen, hydroxyl, esterified hydroxyl in which oxygen atoms may be replaced by sulphur, or an optionally N-substituted carbamoyloxy or thiocarbamoylmercapto group, are prepared by (a) reacting a compound of Formula II wherein R 5 is a group : Z-CH 2 -CO in which Z is an activated ester group and R 2 is as previously defined, with an aminopyridine, or (b) reacting a compound (II) wherein R5 is hydrogen and R 2 is as previously defined, with an acylating agent containing the group R 1 -CH 2 -CO-, or (c) splitting off a protecting group or groups from a compound of Formula I in which any free amino groups and/or carboxyl groups is or are protected by a protective group that can be split off by solvolysis, reduction, nucleophilic exchange or photolysis, if desired with subsequent conversion of a compound (I) in which R 2 has one of its aforesaid meanings into a compound (I) in which R 2 has another such meaning. Pharmaceutical compositions having antibiotic activity comprise a cephalosporin (I) as defined above together with a pharmaceutically suitable carrier. The compound (I) may also be mixed with an animal feedstuff to provide a growthpromoting animal fodder.