MONOBACTAM DERIVATIVE CONTAINING THIOURONIUM SIDE CHAIN

摘要

NEW MATERIAL:A compound shown by formula I (R<1> is methyl or carboxymethyl; R<2>-R<5> are H, lower alkyl or lower alkenyl or both R<2> and R<4> are H and R<3> and R<5> are bonded to form lower alkylene) or a salt thereof. EXAMPLE:( 3R,4R )-3-[ 2-( 2-Amino-4-thiazolyl )-2-methoxyiminoacetamido ]-4-( 2-thiouroniumethyl )-2-oxoazetidine-1-sulfonate. USE:An antibacterial agent against Gram-negative bacteria and a beta-lactamase inhibitor. PREPARATION:A compound shown by formula II (R<11> is methyl or protected carboxymethyl) or a salt thereof is reacted with a thiourea compound shown by formula III usually in an inert solvent preferably at room temperature - 600 deg.C and optionally the reaction product is deprotected.