Section of Organic Chemistry, Department of Chemistry, University of Oslo, Sem Sælands vei 23, 0371 Blindern, Oslo, Norway.
Org Lett. 2021 Feb 5;23(3):1011-1015. doi: 10.1021/acs.orglett.0c04209. Epub 2021 Jan 25.
A Cu(I)-mediated fluoro-deamination method for nucleophilic radiofluorination was devised. The method affords fluorinated aromatic products directly from anilines under both no-carrier added and stoichiometric conditions. Isolated radiochemical yields range from 11% to 81% with high radiochemical purities and a molar activity of 58 MBq/nmol. The reaction conditions were implemented successfully in an automated process for production of ()-4[F]fluorogluthetimide on a radiosynthesis module.
设计了一种铜（I）介导的亲核放射性氟取代反应方法。该方法在无载体添加和化学计量条件下，可直接从苯胺得到氟化芳基产物。放射性化学产率范围为 11%至 81%，具有高放射性化学纯度和 58 MBq/nmol 的摩尔活性。该反应条件已成功应用于放射性合成模块上（）-4[F]氟谷氨酸噻替米的自动化生产过程中。
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