Substd. phenyl-acetamido beta-lactam antibiotics - with e.g. an alkoxy(carbonyl)-alkanoyloxy substit. on the phenyl gp

Substd. phenyl-acetamido beta-lactam antibiotics - with e.g. an alkoxy(carbonyl)-alkanoyloxy substit. on the phenyl gp

beta-Lactams of formula (I) and their esters and salts are new. In the formula R is 1-6C alkyl, or when A is O also H. A is O or OCO. R is H, acetoxy or SHet. Het is 1,2,3-triazol-5-yl, 1-methyl-tetrazol-5-yl, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiadiazol-5-yl. n is 0-8). (I) are antibacterials...

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Hauptverfasser: SEUBERT,JUERGEN,DR, DINGELDEIN,ELVIRA,DR, BERGMANN,ROLF,DR, GOTTSCHLICH,RUDOLF,DR, WAHLIG,HELMUT,DR, GERICKE,ROLF,DR, STREHLOW,WIGHARD,DR, JURASZYK,HORST,DR
Format: Patent
Sprache:eng ; ger
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Zusammenfassung:beta-Lactams of formula (I) and their esters and salts are new. In the formula R is 1-6C alkyl, or when A is O also H. A is O or OCO. R is H, acetoxy or SHet. Het is 1,2,3-triazol-5-yl, 1-methyl-tetrazol-5-yl, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiadiazol-5-yl. n is 0-8). (I) are antibacterials effective against Gram negative and positive species (esp. against Staph. aureus when given orally) and also intermediates for other pharmaceuticals. In an example 6-(2-D-amino-p-ethoxycarbonyloxyphenyl-acetamido) penicillanic acid was prepd. from amoxycillin by reacting first with ethyl acetoacetate and then with ethyl chloroformate.