Automation of the Radiosynthesis of Six Different 18F-labeled radiotracers on the AllinOne

Abstract

BackgroundFast implementation of positron emission tomography (PET) into clinical and preclinical studies highly demands automated synthesis for the preparation of PET radiopharmaceuticals in a safe and reproducible manner. The aim of this study was to develop automated synthesis methods for these six 18F-labeled radiopharmaceuticals produced on a routine basis at the University of Pennsylvania using the AllinOne synthesis module.ResultsThe development of automated syntheses with varying complexity was accomplished including HPLC purification, SPE procedures and final formulation with sterile filtration. The six radiopharmaceuticals were obtained in high yield and high specific activity with full automation on the AllinOne synthesis module under current good manufacturing practice (cGMP) guidelines.ConclusionThe study demonstrates the versatility of this synthesis module for the preparation of a wide variety of 18F-labeled radiopharmaceuticals for PET imaging studies.

Development and radiosynthesis of the first 18F‐labeled inhibitor of monocarboxylate transporters (MCTs)

“…For the radiosynthesis of [ 18 F] FACH , a two‐step approach including radiofluorination and deprotection was applied (Scheme ). An alkali metal fluoride/cryptand complex such as K[ 18 F]F‐K 2.2.2 ‐carbonate is a reagent traditionally used for aliphatic nucleophilic substitution with 18 F‐fluoride . This system is generally strongly basic, which restricts its synthetic utility for base‐sensitive precursors because it generates various side reactions, such as eliminations of alkyl halides or sulfonates to form alkenes .…”

[18F](2S,4R)4-Fluoroglutamine PET Detects Glutamine Pool Size Changes in Triple-Negative Breast Cancer in Response to Glutaminase Inhibition

“…Cells within 50 passages were used for the study. Radiosynthesis of [ 18 F]4F-Gln followed previously established methods (18,22). The minimum specific activity of [ 18 F]4F-Gln at the end of synthesis (EOS) was 40mCi/µmol and the maximal molar dose was 8.75 nanomoles based on the injected dose specified below.…”

Initial experience in synthesis of (2S,4R)‐4‐[18F]fluoroglutamine for clinical application

“…The total radiosynthesis time was about 65 minutes, the decay‐corrected radiochemical yield was 18.0 ± 4.2% (n = 59), the radiochemical purity was greater than 90%, and the optical purity was greater than 95%. When comparing with previously reported HPLC purification method, there was a significant increase in efficiency associated with using the SPE method—by reducing preparation time in synthesis and reducing product loss. In the past 1 year and 5 months, we have performed the procedure for 74 times.…”