ArticleMolecules (Basel, Switzerland)2013
Chelator-accelerated one-pot 'click' labeling of small molecule tracers with 2-[¹⁸F]fluoroethyl azide.
Article in Molecules (Basel, Switzerland), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 16 citations in OpenAlex.
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- A Dual Reporter Iodinated Labeling Reagent for Cancer Positron Emission Tomography Imaging and Fluorescence-Guided Surgery.Journal of medicinal chemistry · 2018Article
- Optimized and Automated Radiosynthesis of [Molecules (Basel, Switzerland) · 2016Article
- Facile purification and click labeling with 2-[Tetrahedron letters · 2015Article
- Development of purine-derived 18F-labeled pro-drug tracers for imaging of MRP1 activity with PET.Journal of medicinal chemistry · 2014Article
- 18F-labeling using click cycloadditions.BioMed research international · 2014Review
- Recent trends in bioorthogonal click-radiolabeling reactions using fluorine-18.Molecules (Basel, Switzerland) · 2013Review
- Labeling single domain antibody fragments withNuclear medicine and biologyArticle
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
2-[¹⁸F]Fluoroethyl azide ([¹⁸F]FEA) can readily be obtained by nucleophilic substitution of 2-azidoethyl-4-toluenesulfonate with [¹⁸F]fluoride (half-life 110 min), and has become widely used as a reagent for 'click' labeling of PET tracers. However, distillation of [18F]FEA is typically required, which is time-consuming and unpractical for routine applications. In addition, copper(I)-catalyzed cycloaddition of [¹⁸F]FEA with non-activated alkynes, and with substrates containing labile functional groups, can be challenging. Herein, we report a highly efficient and practical ligand-accelerated one-pot/two-step method for 'click' labeling of small molecule tracers with [¹⁸F]FEA. The method exploits the ability of the copper(I) ligand bathophenanthrolinedisulfonate to accelerate the rate of the cycloaddition reaction. As a result, alkynes can be added directly to the crude reaction mixture containing [¹⁸F]FEA, and as cyclisation occurs almost immediately at room temperature, the reaction is tolerant to labile functional groups. The method was demonstrated by reacting [¹⁸F]FEA with a series of alkyne-functionalized 6-halopurines to give the corresponding triazoles in 55-76% analytical radiochemical yield.
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