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Effective Preparation of [<sup>18</sup>F]Flumazenil Using Copper-Mediated Late-Stage Radiofluorination of a Stannyl Precursor
oleh: Mohammad B. Haskali, Peter D. Roselt, Terence J. O’Brien, Craig A. Hutton, Idrish Ali, Lucy Vivash, Bianca Jupp
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2022-09-01 |
Deskripsi
(1) Background: [<sup>18</sup>F]Flumazenil <b>1</b> ([<sup>18</sup>F]FMZ) is an established positron emission tomography (PET) radiotracer for the imaging of the gamma-aminobutyric acid (GABA) receptor subtype, GABA<sub>A</sub> in the brain. The production of [<sup>18</sup>F]FMZ <b>1</b> for its clinical use has proven to be challenging, requiring harsh radiochemical conditions, while affording low radiochemical yields. Fully characterized, new methods for the improved production of [<sup>18</sup>F]FMZ <b>1</b> are needed. (2) Methods: We investigate the use of late-stage copper-mediated radiofluorination of aryl stannanes to improve the production of [<sup>18</sup>F]FMZ <b>1</b> that is suitable for clinical use. Mass spectrometry was used to identify the chemical by-products that were produced under the reaction conditions. (3) Results: The radiosynthesis of [<sup>18</sup>F]FMZ <b>1</b> was fully automated using the iPhase FlexLab radiochemistry module, affording a 22.2 ± 2.7% (<i>n</i> = 5) decay-corrected yield after 80 min. [<sup>18</sup>F]FMZ <b>1</b> was obtained with a high radiochemical purity (>98%) and molar activity (247.9 ± 25.9 GBq/µmol). (4) Conclusions: The copper-mediated radiofluorination of the stannyl precursor is an effective strategy for the production of clinically suitable [<sup>18</sup>F]FMZ <b>1</b>.