ArticleChemistryOpen2015
A Practical One-Pot Synthesis of Positron Emission Tomography (PET) Tracers via Nickel-Mediated Radiofluorination.
Article in ChemistryOpen, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Nucleophilic Radiofluorination Using Tri-Molecules (Basel, Switzerland) · 2022Article
- Closing the gap betweenEJNMMI radiopharmacy and chemistry · 2021Review
- Production of 6-l-[Molecules (Basel, Switzerland) · 2021Article
- Recent advances in radiotracers targeting norepinephrine transporter: structural development and radiolabeling improvements.Journal of neural transmission (Vienna, Austria : 1996) · 2020Review
- Harnessing Ionic Interactions and Hydrogen Bonding for Nucleophilic Fluorination.Molecules (Basel, Switzerland) · 2020Review
- Fast and efficient copper-mediatedEJNMMI radiopharmacy and chemistry · 2019Article
- Alcohol-Supported Cu-MediatedMolecules (Basel, Switzerland) · 2019Article
- Radiosynthesis of the norepinephrine transporter tracer [Journal of labelled compounds & radiopharmaceuticals · 2019Article
- Chemistry for Positron Emission Tomography: Recent Advances inAngewandte Chemie (International ed. in English) · 2019Review
- A Practical Method for the Preparation ofMolecules (Basel, Switzerland) · 2017Article
- Improved GMP-compliant multi-dose production and quality control of 6-[EJNMMI radiopharmacy and chemistry · 2017Article
- A Transmetalation Reaction Enables the Synthesis of [Organometallics · 2016Article
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Authors and funding
8 authors.
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No grant is acknowledged in the PubMed record.
Abstract
Recently a novel method for the preparation of (18)F-labeled arenes via oxidative [(18)F]fluorination of easily accessible and sufficiently stable nickel complexes with [(18)F]fluoride under exceptionally mild reaction conditions was published. The suitability of this procedure for the routine preparation of clinically relevant positron emission tomography (PET) tracers, 6-[(18)F]fluorodopamine (6-[(18)F]FDA), 6-[(18)F]fluoro-l-DOPA (6-[(18)F]FDOPA) and 6-[(18)F]fluoro-m-tyrosine (6-[(18)F]FMT), was evaluated. The originally published base-free method was inoperative. However, a "low base" protocol afforded protected radiolabeled intermediates in radiochemical conversions (RCCs) of 5-18 %. The subsequent deprotection step proceeded almost quantitatively (>95 %). The simple one-pot two-step procedure allowed the preparation of clinical doses of 6-[(18)F]FDA and 6-[(18)F]FDOPA within 50 min (12 and 7 % radiochemical yield, respectively). In an unilateral rat model of Parkinsons disease, 6-[(18)F]FDOPA with high specific activity (175 GBq μmol(-1)) prepared using the described nickel-mediated radiofluorination was compared to 6-[(18)F]FDOPA with low specific activity (30 MBq μmol(-1)) produced via conventional electrophilic radiofluorination. Unexpectedly both tracer variants displayed very similar in vivo properties with respect to signal-to-noise ratio and brain distribution, and consequently, the quality of the obtained PET images was almost identical.
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