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Efficient 125I-radiolabeling of biomolecules using a strain-promoted oxidation-controlled cyclooctyne–1,2-quinone cycloaddition reaction

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Abstract

We report a novel 1,2-catechol based radioiodinated precursor for radioiodination of bicyclo[6.1.0]nonyne (BCN) installed biologically active molecules using a strain-promoted oxidation-controlled cyclooctyne–1,2-quinone cycloaddition reaction (SPOCQ) under ambient conditions. Compared to the reported methodologies, the new strategy demonstrates some clear advantages, including high in vitro and in vivo stability, high radiochemical yield, and exceptionally fast reaction kinetics at micro-molar concentration.

Graphical abstract: Efficient 125I-radiolabeling of biomolecules using a strain-promoted oxidation-controlled cyclooctyne–1,2-quinone cycloaddition reaction

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Publication details

The article was received on 18 Nov 2019, accepted on 27 Nov 2019 and first published on 30 Nov 2019


Article type: Communication
DOI: 10.1039/C9CC08982A
Chem. Commun., 2020, Advance Article

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    Efficient 125I-radiolabeling of biomolecules using a strain-promoted oxidation-controlled cyclooctyne–1,2-quinone cycloaddition reaction

    S. Mushtaq and S. H. Park, Chem. Commun., 2020, Advance Article , DOI: 10.1039/C9CC08982A

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