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Background: [18F]AV1451 is a commonly used radiotracer for imaging tau deposits in Alzheimer’s disease (AD) and related non-AD tauopathies. Existing radiosyntheses of [18F]AV1451 require complex purifications to provide doses suitable for use in clinical imaging studies. To address this issue, we have modified the synthesis of [18F]AV1451 to use only 0.5 mg precursor, optimized the Boc-deprotection step and developed a simplified method for HPLC purification of the radiotracer. Results: An optimized [18F]AV1451 synthesis using a TRACERLab FXFN module led to high radiochemical yield (202 ± 57 mCi per synthesis) and doses with excellent radiochemical purity (98 ± 1%) and good specific activity (2521 ± 623 Ci/mmol). Conclusion: An updated and operationally simple synthesis of [18F]AV1451 has been developed that is fully automated and prepares radiotracer doses suitable for use in clinical tau PET studies.
Mossine, A. V., Brooks, A. F., Henderson, B. D., Hockley, B. G., Frey, K. A., & Scott, P. J. H. (2017). An updated radiosynthesis of [18F]AV1451 for tau PET imaging. EJNMMI Radiopharmacy and Chemistry, 2(1). https://doi.org/10.1186/s41181-017-0027-7