串联铱催化的芳烃C-H键硼化/铜介导的[F]TBAF对芳烃C-H键的放射性氟化反应
Tandem Iridium-Catalyzed C-H Borylation/Copper-Mediated Radiofluorination of Aromatic C-H Bonds with [F]TBAF.
作者信息
Morales Maria, Preshlock Sean, Sharninghausen Liam S, Wright Jay S, Brooks Allen F, Sanford Melanie S, Scott Peter J H
机构信息
Department of Chemistry, University of Michigan, Ann Arbor, MI, USA.
Department of Radiology, University of Michigan, Ann Arbor, MI, USA.
出版信息
Methods Mol Biol. 2024;2729:45-53. doi: 10.1007/978-1-0716-3499-8_4.
Abstract
Direct C-H functionalization of (hetero)aromatic C-H bonds with iridium-catalyzed borylation followed by copper-mediated radiofluorination of the in situ generated organoboronates affords fluorine-18 labeled aromatics in high radiochemical conversions and meta-selectivities. This protocol describes the benchtop reaction assembly of the C-H borylation and radiofluorination steps, which can be utilized for the fluorine-18 labeling of densely functionalized bioactive scaffolds.
摘要
通过铱催化的硼化反应对（杂）芳族C-H键进行直接C-H官能化，然后对原位生成的有机硼酸酯进行铜介导的放射性氟化反应，可在高放射化学转化率和间位选择性下得到氟-18标记的芳烃。本方案描述了C-H硼化和放射性氟化步骤的台式反应组装，可用于对密集官能化的生物活性支架进行氟-18标记。
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