| 摘要 |
Penicillins of Formula I <FORM:1064893/C2/1> and non-toxic salts thereof, wherein R is a substituted or unsubstituted alkyl, aralkyl, aryl or heterocyclic group, are prepared by reacting with a basic reagent a N-protected penicillin of Formula II <FORM:1064893/C2/2> wherein R is as above, X is a divalent saturated hydrocarbon radical containing 2 to 6 carbon atoms linked to the groups on either side through adjacent carbon atoms and R1 is a substituted or unsubstituted alkyl, aralkyl or aryl group or a non-toxic salt thereof. Preferably X is ethylene and R1 is p-tolyl, e.g. 6-[D-a -(2-p-toluene sulphonyl ethoxycarbonylamino) - a - phenylacetamido] penicillanic acid. The reaction may be carried out in an aqueous solution of pH 8-11.5, using a base such as a tertiary aliphatic amine. Alternatively, the N-protected penicillin (II) may be treated with an alkali metal hydroxide or alkoxide or metalloorganic compound in an anhydrous organic solvent to produce a carbamate salt of formula <FORM:1064893/C2/3> where M is a metal radical, which is then converted to the aminopenicillin (I) by treatment with acid. |
