Photoredox methods for radiocyanation of arenes and use thereof

Abstract

Carbon is one of the most common elements in bioactive organic compounds. Theoretically, nearly all carbon-based organic functional groups can be labeled with 11C if an appropriate 11C-synthon is developed and utilized. Although there are various reports on developing PET agents based on alkyl [11C]nitriles, efficient and facile cyanation of arenes with radioisotope-containing reagents, particularly electron-rich arenes, still requires further improvements. The organic photoredox-catalyzed cyanation method reported herein introduces a [11C]nitrile quickly with high radiochemical conversion (RCC) in a metal-free manner, which can also be further diversified to other functional groups such as [11C]carboxylic acids, [11C]amides, and [11C]alkyl amines.

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