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Issue 39, 2018
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Azlactone-based heterobifunctional linkers with orthogonal clickable groups: efficient tools for bioconjugation with complete atom economy

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Abstract

We report the efficient synthesis of a series of new azlactone-based heterofunctional linkers bearing two orthogonal clickable groups that proceed with full atom economy. These new linkers comprise an azlactone (oxazolone) group that quickly reacts with amino groups in biologically relevant medium without byproduct elimination and a (bio)orthogonal handle which further undergoes facile and selective click reactions such as thiol–ene coupling, Diels–Alder or azide–alkyne cycloadditions. As an example, the application of this methodology to lysozyme PEGylation in aqueous medium is described.

Graphical abstract: Azlactone-based heterobifunctional linkers with orthogonal clickable groups: efficient tools for bioconjugation with complete atom economy

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Publication details

The article was received on 26 Jul 2018, accepted on 19 Sep 2018 and first published on 19 Sep 2018


Article type: Communication
DOI: 10.1039/C8OB01807C
Citation: Org. Biomol. Chem., 2018,16, 7124-7128
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    Azlactone-based heterobifunctional linkers with orthogonal clickable groups: efficient tools for bioconjugation with complete atom economy

    H. T. Ho, A. Bénard, G. Forcher, M. Le Bohec, V. Montembault, S. Pascual and L. Fontaine, Org. Biomol. Chem., 2018, 16, 7124
    DOI: 10.1039/C8OB01807C

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