Department of Radiology, University of Michigan, 1301 Catherine St, Ann Arbor, MI, 48109, USA.
Department of Chemistry, The University of Michigan, 930 North University Ave, Ann Arbor, MI, 48109, USA.
Angew Chem Int Ed Engl. 2019 Mar 4;58(10):3119-3122. doi: 10.1002/anie.201812701. Epub 2019 Jan 18.
A Cu-mediated ortho-C-H radiofluorination of aromatic carboxylic acids that are protected as 8-aminoquinoline benzamides is described. The method uses K F and is compatible with a wide range of functional groups. The reaction is showcased in the high specific activity automated synthesis of the RARβ2 agonist [ F]AC261066.
描述了一种铜介导的保护为 8-氨基喹啉苯甲酰胺的芳基羧酸的邻位 C-H 放射性氟代反应。该方法使用 KF,与广泛的官能团兼容。该反应在 RARβ2 激动剂[F]AC261066的高比活度自动化合成中得到了展示。