FREMGANGSMADE TIL FREMSTILLING AF PENICILLANSYRE-OG CEPHALOSPORANSYREDERIVATER

This invention relates to a process for the preparation of acid amides having the formula (I) or their salts (I) wherein R1 is hydrogen or an easily removable ester-forming or salt-forming group, preferably a trialkylamine, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl...

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Bibliographische Detailangaben
Hauptverfasser: SOMFAI E, HUHN M, SZABO G, RESOFSZKI G
Format: Patent
Sprache:dan
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Zusammenfassung:This invention relates to a process for the preparation of acid amides having the formula (I) or their salts (I) wherein R1 is hydrogen or an easily removable ester-forming or salt-forming group, preferably a trialkylamine, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group, R2 is hydrogen, alkyl group, alkenyl group, alkyl group having an aryl or heterocyclic (preferably furyl or thienyl) - substituent, an aryl group having an alkyl substituent (preferably xylyl), or an aryl, aralkyl or heterocyclic group (preferably a phenyl, thienyl, or furyl group) which can have one or more substituents, R3 is hydrogen, or substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, and X is a group of one of the formulae according to the invention an amine of the formula (II), (II) wherein R4 is an easily removable ester-forming group, preferably a trialkylamino, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group, or a salt formed preferably with an alkali metal or a trialkylamine, is acylated with an ester of the formula (III), (III) wherein R5 is a substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, and, if desired, substituents R4 and/or R5 of the obtained product can be split off, and/or, if desired, the obtained product is converted into its salt or a salt is converted into the free acid.