Silver-Mediated 18F-Labeling of Aryl-CF3 and Aryl-CHF2 with 18F-Fluoride
Silver-Mediated 18F-Labeling of Aryl-CF3 and Aryl-CHF2 with 18F-Fluoride
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DOI：
10.1055/s-0035-1560592
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发表时间：
2016-01-01
期刊：
影响因子：
2
通讯作者：
Gouverneur, Veronique
中科院分区：
文献类型：
--
作者：
Verhoog, Stefan;Pfeifer, Lukas;Gouverneur, Veronique
我们报道了利用银介导的卤素与[F-18]氟化物的交换，从芳基CF(2)Br和芳基CHFCl前体合成了[F-18]芳基CF(3)和[F-18]芳基CHF(2)衍生物。在没有 Ag(I)OTf 的情况下，这两类底物在室温下都不会发生反应；该结果证明了银 (I) 作为在非常温和的条件下诱导 F-18 掺入的手段的有益作用。
We report the synthesis of [F-18]arylCF(3) and [F-18]arylCHF(2) derivatives from arylCF(2)Br and arylCHFCl precursors applying a silver-mediated halogen exchange with [F-18]fluoride. In the absence of Ag(I)OTf, no reaction takes place at room temperature for both classes of substrates; this result demonstrates the beneficial role of silver(I) as a means to induce F-18-incorporation under very mild conditions.