AZETIDINE DERIVATIVE AND ITS PREPARATION

摘要

NEW MATERIAL:A 1-sulfo-oxoazetidine derivative of formula II (R1 is amino which may be acylated or protected; X is H or methoxy). EXAMPLE:Sodium 3-[ 2-( 2-amino-4-thiazoyl )-2-methoxyiminoacetamido ]-2-oxoazetidine-1-sulfonate. USE:Antibacterial agent effetive to some kinds of Gram-positive and Gram-negative bacteria. Its acute toxicity is 500mg/kg. PROCESS:For example, the compound of formula I can be prepared by the sulfonation reaction of the 2-oxoazetidine derivative of formula II', which can be obtained from a penicillin compound of formula V (R4 is ester residue such as methyl, ethyl, etc.) according to the reaction formulas.