ArticleJournal of nuclear medicine : official publication, Society of Nuclear Medicine2015
Iodonium ylide-mediated radiofluorination of 18F-FPEB and validation for human use.
Article in Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed.
- Recent advances in [Nuclear medicine and biology · 2026Review
- Triflyl [Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- State of the art procedures towards reactive [EJNMMI radiopharmacy and chemistry · 2023Review
- Detrimental impact of aqueous mobile phases on 18F-labelled radiopharmaceutical analysisAnalytical methods : advancing methods and applications · 2023Article
- Revisiting the Radiosynthesis of [Molecules (Basel, Switzerland) · 2020Article
- FacileNature protocols · 2019Article
- Chemistry for Positron Emission Tomography: Recent Advances inAngewandte Chemie (International ed. in English) · 2019Review
- Brain mGluR5 in Shank3BFrontiers in psychiatry · 2019Article
- Ring-Closing Synthesis of Dibenzothiophene Sulfonium Salts and Their Use as Leaving Groups for AromaticJournal of the American Chemical Society · 2018Article
- A first-in-man PET study of [European journal of nuclear medicine and molecular imaging · 2018Article
- In Vitro and in Vivo Evaluation ofJournal of medicinal chemistry · 2018Article
- Hypervalent aryliodine compounds as precursors for radiofluorination.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- A Facile Radiolabeling of [Journal of medicinal chemistry · 2017Article
- Synthesis and preliminary PET imaging ofNature communications · 2017Article
- Copper-Mediated Radiofluorination of Arylstannanes with [Organic letters · 2016Article
- Radiosynthesis and preliminary PET evaluation of (18)F-labeled 2-(1-(3-fluorophenyl)-2-oxo-5-(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile for imaging AMPA receptors.Bioorganic & medicinal chemistry letters · 2016Article
- Efficient Pathway for the Preparation of Aryl(isoquinoline)iodonium(III) Salts and Synthesis of Radiofluorinated Isoquinolines.Angewandte Chemie (International ed. in English) · 2016Article
- (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.Chemical Society reviews · 2016Review
- Mechanistic Studies and Radiofluorination of Structurally Diverse Pharmaceuticals with Spirocyclic Iodonium(III) Ylides.Chemical science · 2016Article
- A Transmetalation Reaction Enables the Synthesis of [Organometallics · 2016Article
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7 authors.
Funding
Abstract
unlabelledTranslation of new methodologies for labeling nonactivated aromatic molecules with (18)F remains a challenge. Here, we report a one-step, regioselective, metal-free (18)F-labeling method that uses a hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical (18)F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile ((18)F-FPEB).
methodsAutomated radiosynthesis of (18)F-FPEB was achieved by reaction of the ylide precursor (4 mg) with (18)F-Et4NF in dimethylformamide at 80°C for 5 min and formulated for injection within 1 h.
results(18)F-FPEB was synthesized in 20% ± 5% (n = 3) uncorrected radiochemical yields relative to (18)F-fluoride, with specific activities of 666 ± 51.8 GBq (18 ± 1.4 Ci)/μmol at the end of synthesis and was validated for human use.
conclusionRadiofluorination of iodonium (III) ylides proved to be an efficient radiosynthetic strategy for synthesis of (18)F-labeled radiopharmaceuticals.
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