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"In-loop" 18 F-fluorination: A proof-of-concept study
Kenneth Dahl1, Armando Garcia1, Nickeisha A Stephenson1,2,3
1Azrieli Centre for Neuro-Radiochemistry, Research Imaging Centre, Centre for Addiction and Mental Health, Toronto, Ontario, Canada.
Journal of Labelled Compounds & Radiopharmaceuticals
|May 15, 2019
Summary
A new "in-loop" radiofluorination method using fluorine-18 (18F) triflyl fluoride offers a cost-efficient and robust way to produce radiopharmaceuticals like [18F]T807 and [18F]FEPPA.
Area of Science:
- Radiochemistry
- Nuclear Medicine
- Pharmaceutical Manufacturing
Background:
- High demand for cost-efficient and robust manufacturing of fluorine-18 (18F) radiopharmaceuticals.
- Existing methods for radiofluorination can be resource-intensive.
Purpose of the Study:
- To develop and validate a novel "in-loop" radiofluorination method.
- To utilize [18F]triflyl fluoride as a labeling agent for efficient radiotracer synthesis.
Main Methods:
- Optimization of the "in-loop" [18F]fluorination using 1,4-dinitrobenzene.
- Application of the method for automated radiosynthesis of [18F]T807 and [18F]FEPPA.
Main Results:
- Successful synthesis of [18F]T807 and [18F]FEPPA with non-decay corrected radiochemical yields of 27% and 29%, respectively.
- Synthesis times of 65 minutes for [18F]T807 and 55 minutes for [18F]FEPPA.
- High radiochemical purity (>99%) and molar activity (>350 GBq/μmol) achieved.
Conclusions:
- The novel "in-loop" radiofluorination method is simple, efficient, and reliable.
- This approach provides equal or superior yields compared to conventional vial-based reactions.
- Enables dependable production of radiofluorinated compounds and radiopharmaceuticals.