Abstract
A simple synthetic method for deprotection of the N- and O-carbobenzoxy groups (Cbz) of the desosamine sugar moiety of ketolides is reported. This deprotection method is applicable to the synthesis of a variety of ketolide analogues with various 9-iminoether moieties in good to moderate yield. Among the ketolide derivatives prepared by this method, compound 7g with a quinoline-6-yl moiety showed potent activity against erythromycin-resistant pathogens as well as Haemophilus influenzae.
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Iwaki, T., Nomura, T., Narukawa, Y. et al. A Simple Method for Deprotection of the N- and O-Carbobenzoxy Groups and N-Methylation of the Desosamine Sugar Moiety of Ketolides. J Antibiot 58, 679–685 (2005). https://doi.org/10.1038/ja.2005.93
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DOI: https://doi.org/10.1038/ja.2005.93