Penicillin derivative

The invention relates to acetoxymethylbenzylpenicillin, which is effective orally. Acetoxymethyl benzylpenicillin is prepared by condensing acetoxymethyl halide e.g. bromide with benzyl penicillin, especially in the form of a salt thereof, in the presence of a solvent such as dimethyl formamide. It...

Full description

Saved in:
Bibliographic Details
Main Authors JANSEN ALEXANDER B. A, RUSSELL TREVOR J
Format Patent
LanguageEnglish
Published 10.05.1966
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online AccessGet full text

Cover

More Information
Summary:The invention relates to acetoxymethylbenzylpenicillin, which is effective orally. Acetoxymethyl benzylpenicillin is prepared by condensing acetoxymethyl halide e.g. bromide with benzyl penicillin, especially in the form of a salt thereof, in the presence of a solvent such as dimethyl formamide. It may be crystallized from chloroform or isopropyl alcohol. Acetoxymethyl halides are prepared by heating an acetyl halide with paraformaldehyde in the presence of anhydrous zinc chloride and recovering the acetoxymethyl halide by distillation. Pharmaceutical compositions for oral use comprise acetoxymethyl benzylpenicillin and a carrier. The composition may take the form of powders, tablets, granules, capsules, troches, cachets, solutions, suspensions and emulsions. Other penicillins may be present. On oral administration, sustained high blood levels of penicillin are obtained.
Bibliography:Application Number: US19640370687