Tandem Iridium-Catalyzed C-H Borylation/Copper-Mediated Radiofluorination of Aromatic C-H Bonds with [18F]TBAF.
Tandem Iridium-Catalyzed C-H Borylation/Copper-Mediated Radiofluorination of Aromatic C-H Bonds with [18F]TBAF.
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[18F]TBAF 串联铱催化 C-H 硼化/铜介导的芳香族 C-H 键放射性氟化。
DOI：
10.1007/978-1-0716-3499-8_4
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发表时间：
2024
期刊：
影响因子：
--
通讯作者：
Scott,PeterJH
中科院分区：
文献类型：
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作者：
Morales,Maria;Preshlock,Sean;Sharninghausen,LiamS;Wright,JayS;Brooks,AllenF;Sanford,MelanieS;Scott,PeterJH
通过铱催化的硼化反应直接将杂芳环C-H键官能化，然后通过铜介导的原位生成的有机硼酸酯的放射性取代，以高的放射化学转化率和间位选择性得到氟-18标记的芳族化合物。该方案描述了C-H硼基化和放射性同位素标记步骤的台式反应组装，其可用于密集功能化生物活性支架的氟-18标记。
Direct C–H functionalization of (hetero)aromatic C–H bonds with iridium-catalyzed borylation followed by copper-mediated radiofluorination of thein situgenerated organoboronates affords fluorine-18 labeled aromatics in high radiochemical conversions andmeta-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.