Department of Molecular and Medical Pharmacology and Crump Institute for Molecular Imaging, David Geffen School of Medicine, University of California, Los Angeles, Los Angeles, CA, 90095, USA.
Department of Chemistry and Biochemistry, and Department of Chemical and Biomolecular Engineering, University of California, Los Angeles, Los Angeles, CA, 90095, USA.
Angew Chem Int Ed Engl. 2017 Oct 9;56(42):13006-13010. doi: 10.1002/anie.201707274. Epub 2017 Sep 7.
A practical method for radiofluorination of anilines with [ F]fluoride via N-arylsydnone intermediates is described. These precursors are stable, easy to handle and facilitate direct and regioselective F-labeling to prepare [ F]fluoroarenes. The value of this methodology is further highlighted by successful application to prepare an F-labeled neuropeptide.
描述了一种通过 N-芳基-1,2-二氢-2-氧代-3H-吡咯并[3,4-b]吡啶中间体实现苯胺[ F]放射性氟化的实用方法。这些前体稳定、易于处理，并有利于直接和区域选择性的 F-标记以制备[ F]氟代芳烃。该方法的价值通过成功应用于制备 F 标记的神经肽得到进一步强调。
