Direct diazo-transfer reaction on β-lactam: Synthesis and preliminary biological activities of 6-triazolylpenicillanic acids

PC Chen, RE Wharton, PA Patel, AK Oyelere

文献索引：Chen, Po C.; Wharton, Rebekah E.; Patel, Pratiq A.; Oyelere, Adegboyega K. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 23 p. 7288 - 7300

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被引用次数: 18

摘要

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 ...