ArticleMolecular imaging and biology2014
Fully automated radiosynthesis of 2-[18F]fludarabine for PET imaging of low-grade lymphoma.
Article in Molecular imaging and biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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7 citing papers in PubMed, 14 citations in OpenAlex.
- State of the art procedures towards reactive [EJNMMI radiopharmacy and chemistry · 2023Review
- Positron emission tomography and magnetic resonance imaging in primary central nervous system lymphoma-a narrative review.Annals of lymphoma · 2021Article
- [Frontiers in medicine · 2019Review
- [Theranostics · 2018Article
- [18F]Fludarabine-PET in a murine model of multiple myeloma.PloS one · 2017Article
- Evaluation of the specificity of [(18)F]fludarabine PET/CT in a xenograft model of follicular lymphoma: comparison with [(18)F]FDG and impact of rituximab therapy.EJNMMI research · 2015Article
- 2-[18F]fludarabine, a novel positron emission tomography (PET) tracer for imaging lymphoma: a micro-PET study in murine models.Molecular imaging and biology · 2014Article
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Authors and funding
8 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeAn efficient and fully automated radiosynthesis of 2-[(18)F]fluoro-9-β-D-arabinofuranosyl-adenine (2-[(18)F]fludarabine, [(18)F]-5) based on a GE TRACERlab™ FX-FN module has been developed. PROCEDURES: A 2-nitro purine derivative 3 was developed as precursor for labeling with fluorine-18. The radiosynthesis of [(18)F]-5 was performed in two steps in a single reactor with an intermediary purification on Sep-Pak® silica which involved the addition of a three-way valve on the original module. After hydrolysis, [(18)F]-5 was purified by semi-preparative high-pressure liquid chromatography (HPLC) and a quality control was established.
resultsThe labeling precursor 3 was obtained in 45% overall yield. Nucleophilic substitution with K(18)F/K2.2.2 afforded protected 2-[(18)F]fludarabine ([(18)F]-4) in 73 ± 4%, radiochemical yield (decay corrected to the end of bombardment (EOB)) and based on the initial [(18)F]F(-) activity. An aqueous ammonia/methanol solution was used for the deprotection reaction and gave the desired [(18)F]-5 in 67 ± 3% yield after 20 min at 70 °C based on HPLC profile.
conclusionsThe process afforded pure 2-[(18)F]fludarabine in 48 ± 3% yield (decay corrected to the EOB) in 85 min, with a specific activity of 310 ± 72 GBq/μmol at the end of synthesis (EOS) and a radiochemical purity up to 99%.
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