THE SYNTHESIS OF 1- (3', 4'-DIMETHOXY) BENZOYL-3-AMIDO-4-SUBSTITUTED PHENYL-2-AZETIDINONES AND THEIR BETA-LACTAMASE INHIBITION ACTIVITIES

Fourteen novel title compounds were. designed and synthesized through cyclocondensation, deprotection, acylation and oxidative reactions. Their chemical structures were identified by elemental analysis, IR and mass spectra. The cis-configuration of these beta-lactams were determined by coupling constants in 360 MC ¹HNMR spectra.The inhibition activities of these compounds to acetobacter beta-lactamase were testedprcliminarily. Eleven of them exhibited marked activities. Among them, the inhibiting activities of Ⅲe-1 and Ⅲg-1 are twice as that of sulbactam.