PURPOSE: To obtain a compound which is useful as intermediate of a new β- lactam antibiotic having antimicrobial activity for microorganisms of both region of Gram negative and Gram position, and useful as antimicrobial agent.
CONSTITUTION: The compound of formula I, for example, (S)-3-amino-2-oxo-1- azetidinesulfonic acid is obtained by sulfonating a compound of formula II, deprotecting the obtained compound and treating the resultant compound of formula III (M+ is H, cation) with an acid such as formic acid. In the formula I, R2 is H, a 1-4C alkoxy; R3, R4 are each H, an alkyl, cycloalkyl, phenyl, substituted phenyl, one of R3 and R4 is H, the other is an alkoxycarbonyl, alken-1-yl, alkyl-1-yl, 2-phenyl-ethenyl, 2-phenyl-ethynyl. The compound is useful for treatment of fungus infectious disease (urethra and respiratory tract infection) of the mammals containing human, and dosage is 1.4-350 mg/kg/day, preferably about 14-100 mg/kg/day.
PARKER WILLIAM LAWRENCE (US)
CIMARUSTI CHRISTOPHER MICHAEL (US)
KOSTER WILLIAM HENRY (US)
SLUSARCHYK WILLIAM ALLEN (US)
FRITZ ALAN WILLIAM (US)
FLOYD DAVID MACK (US)
