Abstract：
(1) Background: [18F]Flumazenil 1 ([18F]FMZ) is an established positron emission tomography (PET) radiotracer for the imaging of the gamma-aminobutyric acid (GABA) receptor subtype, GABAA in the brain. The production of [18F]FMZ 1 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 [18F]FMZ 1 are needed. (2) Methods: We investigate the use of late-stage copper-mediated radiofluorination of aryl stannanes to improve the production of [18F]FMZ 1 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 [18F]FMZ 1 was fully automated using the iPhase FlexLab radiochemistry module, affording a 22.2 ± 2.7% (n = 5) decay-corrected yield after 80 min. [18F]FMZ 1 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 [18F]FMZ 1.
摘要：
（1）背景：[18F]氟马西尼1（[18F]FMZ）是一种已建立的正电子发射断层扫描（PET）放射性示踪剂，用于γ-氨基丁酸（GABA）受体亚型的成像，大脑中的GABAA[18F]FMZ1的生产用于其临床用途已被证明是具有挑战性的，需要苛刻的放射化学条件，同时提供低放射化学产量。充分表征,需要改进[18F]FMZ1生产的新方法。（2）方法：我们研究了使用后期铜介导的芳基锡烷放射性氟化来改善适合临床使用的[18F]FMZ1的产量。质谱用于鉴定在反应条件下产生的化学副产物。（3）结果：使用iPhaseFlexLab放射化学模块完全自动化[18F]FMZ1的放射合成，80分钟后提供22.2±2.7％（n=5）的衰减校正产率。[18F]FMZ1以高放射化学纯度（98％）和摩尔活性（247.9±25.9GBq/µmol）获得。（4）结论：锡烷基前体的铜介导的放射性氟化是生产临床上合适的[18F]FMZ1的有效策略。
