Syntheses of 1β-methylcarbapenems bearing 5-methyl-4- hydroxypyrrolidinone

Abstract

A new series of 1β-methylcarbapenems 1a - d bearing 5-methyl-4-mercaptopyrrolidinone rings has been prepared and evaluated for in vitro antibacterial activity and pharmacokinetic parameters. Most compounds showed excellent antibacterial activity and high stability to dehydropeptidase-1. We have synthesized optically active 5-methyl-4- hydroxypyrrolidinones from enantiomerically pure aziridine esters. © 2002 Pharmaceutical Society of Japan.