Synthesis of <sup>18</sup>F-Labeled Aryl Fluorosulfates via Nucleophilic Radiofluorination
作者:Young-Do Kwon、Min Ho Jeon、Nam Kyu Park、Jeong Kon Seo、Jeongmin Son、Young Hoon Ryu、Sung You Hong、Joong-Hyun Chun
DOI:10.1021/acs.orglett.0c01868
日期:2020.7.17
first SO2F2-free synthesis of aryl [18F]fluorosulfates from both phenolic and isolated aryl imidazylate precursors with cyclotron-produced 18F–. 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 [18F]fluorosulfate.
硫酰氟气体是SO 2 F转移的关键试剂。然而,由于无法获得气态[ 18 F] SO 2 F 2,传统的SO 2 F转移反应具有局限性的18 F-放射化学转化。在此,我们报告了使用回旋加速器生产的18 F –酚和分离的芳基亚氨基磺酸酯前体,首次合成无SO 2 F 2的芳基[ 18 F]氟代硫酸盐–。放射化学收率范围从中等到良好,且具有出色的官能团耐受性。我们的方法的可靠性通过4-乙酰氨基苯基[ 18 F]氟硫酸盐的自动放射合成得到了验证。