NEW MATERIAL:2-(2-Oxopyrrolidin-3-ylthio)-6-(1-hydroxyethyl)-1-- methylcarbapen-2-em-3-carboxylic acid pivaloyloxymethyl ester shown by formula I.
USE: An antimicrobial agent having extremely excellent oral absorption, showing high stability to dehydropeptidase, having low toxicity and high safety.
PREPARATION: First, the oxo group at the 2-position of carbapenem ring of a compound shown by formula II (Y is carboxyl-protecting group) is activated by reaction with benzenesulfonic anhydride in a solvent in the presence of a base and the resultant substance is reacted with a compound shown by formula III in a solvent in the presence of a base at-20 to 40°C. Then the prepared compound shown by formula IV is deprotected and then reacted with a compound shown by formula V in a solvent in the presence of a base at 0-50°C.
KONDO KAZUHIKO
HORIKAWA KOUJI
MATSUSHITA TADAHIRO
YAMAGUCHI TOTARO
