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Issue 3, 2020
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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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Article information


Submitted
18 Nov 2019
Accepted
27 Nov 2019
First published
30 Nov 2019

Chem. Commun., 2020,56, 415-418
Article type
Communication

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, 56, 415
DOI: 10.1039/C9CC08982A

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