[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. 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). 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.

中文翻译：

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用于 tau PET 成像的 [18F] AV1451 的更新放射合成。

[18F]AV1451 是一种常用的放射性示踪剂，用于对阿尔茨海默病 (AD) 和相关的非 AD tau 蛋白病中的 tau 沉积物进行成像。[18F]AV1451 的现有放射合成需要复杂的纯化以提供适用于临床成像研究的剂量。为了解决这个问题，我们修改了 [18F]AV1451 的合成，使其仅使用 0.5 mg 前体，优化了 Boc 去保护步骤，并开发了一种简化的 HPLC 纯化放射性示踪剂的方法。使用 TRACERLab FXFN 模块优化的 [18F] AV1451 合成导致高放射化学产率（每次合成 202 ± 57 mCi）和具有出色放射化学纯度（98 ± 1%）和良好比活性（2521 ± 623 Ci/mmol）的剂量。