Direct C-H Radiocyanation of Arenes via Organic Photoredox Catalysis

Innovative labeling methods to incorporate the shortlived 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 photoredoxmediated 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.

Automated summary

This study reports an innovative labeling method that incorporates the short-lived positron emitter carbon-11 into bioactive molecules using photoredox catalysis. The method is easy to operate and allows for scalable synthesis of the labeled compounds.