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ID: ALA1137505

Journal: Bioorg Med Chem

Title: Direct diazo-transfer reaction on beta-lactam: synthesis and preliminary biological activities of 6-triazolylpenicillanic acids.

Authors: Chen PC, Wharton RE, Patel PA, Oyelere AK.

Abstract: In this study we report the first example of a direct diazo-transfer reaction on readily available 6-aminopenicillanates to give 6-azidopenicillanates in high yield. Subsequent Cu(I)-catalyzed Huisgen cycloaddition between these 6-azidopenicillanates and assorted terminal alkynes facilely furnished 6-triazolylpenicillanic acids. Preliminary biological screening indicates that these triazolylpenicillanic acids possess low to moderate antibacterial activities.

CiteXplore: 17855098

DOI: 10.1016/j.bmc.2007.08.035