Beyzavi M Hassan, Mandal Debashis, Strebl Martin G, Neumann Constanze N, D'Amato Erica M, Chen Junting, Hooker Jacob M, Ritter Tobias
Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, United States.
Athinoula A. Martinos Center for Biomedical Imaging, Massachusetts General Hospital and Harvard Medical School, Charlestown, Massachusetts 02129, United States.
ACS Cent Sci. 2017 Sep 27;3(9):944-948. doi: 10.1021/acscentsci.7b00195. Epub 2017 Aug 3.
The deficiency of robust and practical methods for F-radiofluorination is a bottleneck for positron emission tomography (PET) tracer development. Here, we report the first transition-metal-assisted F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atmosphere, large substrate scope, and translatability to generate doses appropriate for PET imaging.
缺乏用于氟放射性氟化的强大且实用的方法是正电子发射断层扫描（PET）示踪剂开发的一个瓶颈。在此，我们报道了首例过渡金属辅助的酚类F-脱氧氟化反应。该转化反应具有以下优势：以易于获得的酚类作为起始原料、对水分和环境大气具有耐受性、底物范围广以及可转化以生成适用于PET成像的剂量。
