PROCESS FOR PREPARING BIS-ESTERS OF METHANE DIOL WITH 6'-ACYLAMINOPENICILLANIC ACID AND PENICILLANIC ACID 1,1-DIOXIDE

Esters of formula (I) and their salts are new R is H or R1; R1 is a carboxylic acyl gp. Intermediates of formula (V) are also new. (I;R=R1) are hydrolysed in vivo to form penicillanic acid, 1,1-dioxide (II) and the corresp. penicillin (III) and (II) acts as a beta-lactamase inhibitor which potentiat...

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1. Verfasser: BIGHAM ERIC CLEVELAND
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Sprache:eng
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Zusammenfassung:Esters of formula (I) and their salts are new R is H or R1; R1 is a carboxylic acyl gp. Intermediates of formula (V) are also new. (I;R=R1) are hydrolysed in vivo to form penicillanic acid, 1,1-dioxide (II) and the corresp. penicillin (III) and (II) acts as a beta-lactamase inhibitor which potentiates the antibacterial activity of (III), e.g. against S. aureus or E. coli (depending on the nature of R1). (I; R=H) is an intermediate for (I; R = R1). (I) where R is 2-phenylacetyl, 2-phenoxyacetyl, 2-amino-2-phenylacetyl or 2-amino-2-(4-hydroxyphenyl)acetyl is specifically claimed.