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A facile way to assemble a series of potent acylide derivatives against both macrolide-susceptible and macrolide-resistant strains was reported.
A series of novel acylide derivatives have been synthesized from erythromycin A via a facile procedure. By applying this procedure, cyclic carbonation to C-11,12 position, acylation to C-3 hydroxyl, and deprotection provided the desired acylides. These compounds showed antibacterial activity against both macrolide-susceptible strains and macrolide-resistant strains. Because of existence of 6-
O-allyl substitution, these derivatives can be used as intermediates for further structural modification.