Derivatives of 1 - penicillanic acid oxide, devoid of Therapeutic activity, useful as Intermediates in the preparation of 1.1 - penicillanic acid dioxide pharmaceutically ActiveProcedure for preparing such intermediaries and Procedure for preparing 1,1 dioxides - penicillanic acid pharmaceutically active on such intermediaries

摘要

1,1-Dioxides of penicillanic acid and esters are described which are useful as beta -lactamase inhibitors. These compounds are 1,1-dioxides of penicillanic acid and of corresponding esters which are easily hydrolysable in vivo, derivatives of penicillanic acid 1,1-dioxide, the carboxyl radical of which is protected by a standard protective group of the carboxyl radical of penicillins, which are useful intermediates for the synthesis of penicillanic acid 1,1-dioxide, and 1-oxides of penicillanic acid and of certain of its esters which are useful as chemical intermediates for the synthesis of penicillanic acid 1,1-dioxide and of its esters. These 1,1-dioxides of penicillanic acid and esters are antibacterial agents, also capable of increasing the effectiveness of various antibiotics of the beta -lactam type with respect to bacteria which produce beta -lactamase.