Chen Wei, Wu Xuedan, McManus Joshua B, Bida Gerald T, Li Kang-Po, Wu Zhanhong, Nicewicz David A, Li Zibo
Biomedical Research Imaging Center, Department of Radiology, and UNC Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Department of Chemistry, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Org Lett. 2022 Dec 23;24(50):9316-9321. doi: 10.1021/acs.orglett.2c03940. Epub 2022 Dec 12.
Innovative labeling methods to incorporate the short-lived positron emitter carbon-11(C) into bioactive molecules are attractive for positron emission tomography (PET) tracer discovery. Herein, we report a direct C-H radiocyanation method that incorporates [C]cyanide (CN) to a series of functional electron-rich arenes via photoredox catalysis. This photoredox-mediated radiocyanation can proceed in an aerobic environment and is not moisture sensitive, which allows for ease of reaction setup and for scalable synthesis of C-aryl nitriles from readily available precursors.
将短寿命正电子发射体碳-11（¹¹C）掺入生物活性分子的创新标记方法对于正电子发射断层扫描（PET）示踪剂的发现具有吸引力。在此，我们报告了一种直接的C-H放射性氰化方法，该方法通过光氧化还原催化将[¹¹C]氰化物（¹¹CN）掺入一系列富电子的官能芳烃中。这种光氧化还原介导的放射性氰化可以在有氧环境中进行，并且对水分不敏感，这使得反应设置容易，并且能够从容易获得的前体可扩展地合成C-芳基腈。
