Synthesis of [18F]Fluoroarenes by Nucleophilic Radiofluorination of N-Arylsydnones

Synthesis of [18F]Fluoroarenes by Nucleophilic Radiofluorination of N-Arylsydnones
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DOI:
10.1002/anie.201707274
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发表时间:
2017-10-09
影响因子:
16.6
通讯作者:
Murphy, Jennifer M.
Murphy, Jennifer M.
中科院分区:
化学1区
文献类型:
--
作者:
Narayanam, Maruthi Kumar;Ma, Gaoyuan;Murphy, Jennifer M.

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本文介绍了一种用[F-18]氟化物通过N-芳基悉尼酮中间体放射性取代苯胺的实用方法。这些前体是稳定的,易于处理,并促进直接和区域选择性的F-18-标记以制备[F-18]氟代芳烃。成功应用于制备F-18标记的神经肽进一步突出了这种方法的价值。
A practical method for radiofluorination of anilines with [F-18]fluoride via N-arylsydnone intermediates is described. These precursors are stable, easy to handle and facilitate direct and regioselective F-18-labeling to prepare [F-18]fluoroarenes. The value of this methodology is further highlighted by successful application to prepare an F-18-labeled neuropeptide.