CARBAPENEM-3-CARBOXYLIC ACID DERIVATIVE AND PENEM-3-CARBOXYLIC ACID DERIVATIVE AND THEIR PREPARATION

摘要

NEW MATERIAL:A compound of formula I [R1 is H, alkyl, alkoxy, R5A-group (R5 is hydroxyl, alkoxy, acyloxy; A is trifluoromethyl, alkylene); R2 is lower alkyl; R3 is 4-8-membered cyclic aliphatic amine which may contain O and/or S atoms in the ring; R4 is H, carboxyl-protecting group; X is methylene, thio] or its salt. EXAMPLE:( 5R,6S )-2-[ 1-( Pyrrolidin-3-yl )ethylthio ]-6-[ (R)-1-hydroxyethyl]carbapenem-3-carboxylic acid. USE:Antibacterial. PREPARATION:For example, the reaction of a compound of formula II (R8 is H, alkyl; R10 is protecting group) with a sulfonic acid in the presence of a base is followed by the reaction with a mercaptan of formula III (R9 is R3 protected in its N atom) and deprotection to give the compound of formula I .