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Published on: May 21, 2019
Direct C-H Radiocyanation of Arenes via Organic Photoredox Catalysis
Wei Chen1, Xuedan Wu1, Joshua B McManus2
1Biomedical 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.
Abstract:
Innovative labeling methods to incorporate the short-lived positron emitter carbon-11(11C) into bioactive molecules are attractive for positron emission tomography (PET) tracer discovery. Herein, we report a direct C-H radiocyanation method that incorporates [11C]cyanide (11CN-) 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 11C-aryl nitriles from readily available precursors.
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