An automated radiosynthesis of carbon‐11 positron emission tomography radiotracer [11C]UCB‐J for imaging the synaptic density biomarker synaptic vesicle glycoprotein SV2A was established using Synthra RNPlus synthesizer. Commercially available trifluoroborate UCB‐J analogue was used as a radiolabelling precursor, and the desired radiolabelled product was isolated in 11 ± 2% (n = 7) nondecay corrected radiochemical yield and formulated as a 10% EtOH solution in saline with molar activities of 20 to 100 GBq/μmol. The method was based upon the palladium(0)‐mediated Suzuki cross‐coupling reaction and [11C]CH3I as a radiolabelling synthon. The isolated product was cGMP compliant as demonstrated by the results of quality control analysis.

中文翻译：

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[11 C]UCB-J 的自动放射合成用于通过正电子发射断层扫描成像突触密度


使用 Synthra RNPlus 合成仪建立了碳 11 正电子发射断层扫描放射性示踪剂 [11C]UCB-J 的自动放射合成，用于对突触密度生物标志物突触小泡糖蛋白 SV2A 进行成像。市售的三氟硼酸盐 UCB-J 类似物用作放射性标记前体，所需的放射性标记产物以 11 ± 2% (n = 7) 非衰变校正放射化学产率分离，并配制成摩尔活度为 20 的 10% EtOH 盐水溶液。至 100 GBq/μmol。该方法基于钯 (0) 介导的 Suzuki 交叉偶联反应和作为放射性标记合成子的 [11C]CH3I。质量控制分析结果表明，分离出的产品符合 cGMP 标准。