6533b7d6fe1ef96bd12665ad
RESEARCH PRODUCT
Improved automated synthesis of [18F]fluoroethylcholine as a radiotracer for cancer imaging.
I. KletteR.p. BaumAndreas BaumanMarkus PielR. WortmannS. HöhnemannFrank Röschsubject
Fluorine RadioisotopesClinical BiochemistryIodidePharmaceutical ScienceCancer imagingAlkylationBiochemistryChemical synthesisSensitivity and SpecificityCholineNeoplasmsDrug DiscoverymedicineMolecular BiologyChromatography High Pressure LiquidFluoroethylcholinechemistry.chemical_classificationmedicine.diagnostic_test18F-FluoroethylcholineMolecular StructureChemistryOrganic ChemistryRadiochemistryBiochemistryFully automatedPositron emission tomographyMolecular Medicinedescription
[(18)F]Fluoroethylcholine has been recently introduced as a promising (18)F-labelled analogue of [(11)C]choline which had been previously described as a tracer for metabolic cancer imaging with positron emission tomography (PET). Due to the practical advantages of using the longer-lived radioisotope (18)F (t(1/2)=110 min), offering the opportunity of a more widespread clinical application, we established a reliable, fully automated synthesis for its production using a modified, commercially available module. [(18)F]Fluoroethylcholine was prepared from N,N-dimethylaminoethanol by iodide catalyzed alkylation with 1-[(18)F]fluoro-2-tosylethane as alkylating agent, resulting in a total radiochemical yield of 30+/-6% after a synthesis time of 50 min. The specific activity of [(18)F]fluoroethylcholine was >55 GBq/micromol and the radiochemical purity 95-99%.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2007-05-01 | Bioorganicmedicinal chemistry |