Department of Nuclear Medicine, Yonsei University College of Medicine, Seoul 03722, Republic of Korea.
Department of Chemistry, School of Energy and Chemical Engineering, Ulsan National Institute of Science and Technology (UNIST), Ulsan 44919, Republic of Korea.
Org Lett. 2020 Jul 17;22(14):5511-5516. doi: 10.1021/acs.orglett.0c01868. Epub 2020 Jun 26.
Sulfuryl fluoride gas is a key reagent for SOF transfer. However, conventional SOF transfer reactions have limited F-radiochemistry translation, due to the inaccessibility of gaseous [F]SOF. Herein, we report the first SOF-free synthesis of aryl [F]fluorosulfates from both phenolic and isolated aryl imidazylate precursors with cyclotron-produced F. The radiochemical yields ranged from moderate to good with excellent functional group tolerance. The reliability of our approach was validated by the automated radiosynthesis of 4-acetamidophenyl [F]fluorosulfate.
硫酰氟气体是 SOF 转移的关键试剂。然而，由于气态 [F]SOF 难以接近，传统的 SOF 转移反应对 F 放射性化学的转化有限。在此，我们报告了首例使用回旋加速器产生的 F 从酚类和分离的芳基咪唑盐前体制备芳基 [F]氟硫酸酯，无需 SOF。放射性化学产率中等至良好，具有极好的官能团耐受性。我们的方法的可靠性通过自动化合成 4-乙酰氨基苯 [F]氟硫酸酯得到了验证。
