BIS 1,1-ALKANEDIOL ESTERS OF PENICILLIN DERIVATIVES DEGRADABLE IN VIVO INTO BETA-LACTAMS AND BETA-LACTAMASE INHIBITORS:PHARMACEUTICAL COMPOSITIONS

摘要

Novel bis-Esters of 1,1-alkanediols with 6-beta(hydroxymethyl)penicillanic acid 1,1-dioxide and 6-betaacylaminopenicillanic acids are useful as antibacterial agents. Novel intermediates useful for the preparation of these compounds include: haloalkyl, alkylsulfonyloxyalkyl and arylsulfonyloxyalkyl esters of 6-beta-(hydroxymethyl)penicillanic acid and its 1-oxide and 1,1-dioxide; 6-beta-aminopenicillanoyloxyalkyl and 6-beta-(N-protected-D-2-amino-2-phenylacetamido and 2-[4-hydroxyphenyl]acetamido) penicillanoyloxyalkyl esters of 6-beta-(hydroxymethyl)penicillanic acid 1,1-dioxide; and haloalkyl, alkylsulfonyloxyalkyl and arylsulfonyloxyalkyl esters of the 6-bromo-6-(hydroxymethyl)penicillanic acids.