Automated synthesis of 4-[18F]fluoroanisole, [18F]DAA1106 and 4-[18F]FPhe using Cu-mediated radiofluorination under “minimalist” conditions

The application of the “minimalist” approach to Cu-mediated radiofluorination allows the efficient preparation of 18F-labeled arenes regardless of their electronic properties. The implementation of this methodology on a commercially available synthesis module (hotboxthree, Scintomics, Germany) enabl...

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Bibliographic Details
Published in:Applied radiation and isotopes 2016-09, Vol.115, p.133-137
Main Authors: Zischler, Johannes, Krapf, Philipp, Richarz, Raphael, Zlatopolskiy, Boris D., Neumaier, Bernd
Format: Article
Language:English
Subjects:
[18F]Fluoride
Automated radiosynthesis
Cu-mediated radiolabeling
Minimalist approach
PET-tracers
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Summary:The application of the “minimalist” approach to Cu-mediated radiofluorination allows the efficient preparation of 18F-labeled arenes regardless of their electronic properties. The implementation of this methodology on a commercially available synthesis module (hotboxthree, Scintomics, Germany) enabled the automated production of 4-[18F]fluoroanisole as well as the clinically relevant PET-tracers, 4-[18F]FPhe and [18F]DAA1106, in radiochemical yields of 41–61% and radiochemical purities of >95% within 30–60min. These results demonstrated the high efficacy and versatility of the developed method that will open up opportunities for a broad application of Cu-mediated radiofluorination in PET-chemistry. •Direct elution of [18F]fluoride from an anion exchange resin with a iodonium salt precursor in MeOH.•Neither azeotropic drying, nor base necessary.•Purification of 4-[18F]fluoroanisole, [18F]DAA1106 and 4-[18F]FPhe using solid phase extraction (SPE).•Preparation of PET tracers in isolated radiochemical yields of 41–61% within 30–60min.
ISSN:0969-8043
1872-9800
DOI:10.1016/j.apradiso.2016.04.030