PROCESS FOR THE CONVERSION OF ALPHA-CARBOARYLOXYBENZYLPENICILLINS TO ALPHA-CARBOXYBENZYLPENICILLINS

摘要

[alpha]-Carboxybenzylpenicillin salts are prepared by the hydrolysis of [alpha]-carbo (benzyl or aryl) oxybenzylpenicillins or salts thereof in aqueous solution buffered at a pH from 8 to 9À5 at 10 to 50 C. The buffer system may be boric acid/ NaOH or KOH, glycine/NaOH or KOH or citric acid/NaOH or KOH. The aryl radical is phenyl, chloro, bromo, fluoro, alkyl, alkoxy, alkanoyl, carboalkoxy, nitro and/or dialkylamino substituted phenyl furyl, quinolyl, methyl substituted quinolyl, phenazinyl, 9,10- anthraquinonyl, phenanthrenequinonyl, anthracenyl, phenanthryl, 1,3-benzodioxolyl, 3-(2- methyl-4-pyronyl), 3-(4-pyronyl), (N-methyl)- pyridyl wherein Y 2 is - or or wherein Z1 is -(CH 2 ) 3 -, -(CH 2 ) 4 - or methyl, chloro or bromo substituted derivatives thereof.