A method for the production of 6 - beta - amidinopenicillansaeure - derivatives

摘要

6 beta -Aminomethyleneaminopenicillanic acid derivatives of the following formula IMAGE are prepared, in which R1 and R2 are identical or different and unbranched or branched aliphatic hydrocarbon radicals or cycloaliphatic hydrocarbon radicals, where R1 and R2 may also form together with the nitrogen atom a heterocyclic radical; R3 is H, alkyl, aralkyl or pivaloyloxymethyl. These compounds are obtained by reacting a corresponding 6-aminopenicillanic ester or trimethylsilyl 6-aminopenicillanate with an appropriate secondary amine. The reaction is carried out in the presence of a condensing agent selected from the group comprising orthoformates, thioorthoformates and 1,1-dichlorodimethyl ether. The reaction is carried out at -5 to +30 DEG C in an organic solvent medium. The resulting derivatives can be used as antibacterial agents.