The preparation of a series of acyloxymethyl esters of D-a-ammobenzylpenicillin (ampicillin) is described. In vitro these esters are hydrolyzed to ampicillin by nonspecific esterases present in serum and various tissues from rat, dog, and man.Experiments performed with the hydrochloride of the pivaloyloxymethyl ester in laboratory animals and healthy volunteers show that this compound, after oral administration, is absorbed far more efficiently than ampicillin. After the absorption the compound is rapidly hydrolyzed to ampicillin with the result that high blood and tissue levels of the latter are attained.

No abstract

No abstract

Das Kaliumsalz (I) wurde mit (II) in siedendem Aceton zum Ester (III) umgesetzt, der über Palladiumkohle hydriert wurde zu (IV).

No abstract