Light‐Driven Radiochemistry with Fluorine‐18, Carbon‐11 and Zirconium‐89

Abstract This review discusses recent advances in light‐driven radiochemistry for three key isotopes: fluorine‐18, carbon‐11, and zirconium‐89, and their applications in positron emission tomography (PET). In the case of fluorine‐18, the predominant approach involves the use of cyclotron‐produced [ 18 F]fluoride or reagents derived thereof. Light serves to activate either the substrate or the fluorine‐18 labeled reagent. Advancements in carbon‐11 photo‐mediated radiochemistry have been leveraged for the radiolabeling of small molecules, achieving various transformations, including 11 C‐methylation, 11 C‐carboxylation, 11 C‐carbonylation, and 11 C‐cyanation. Contrastingly, zirconium‐89 photo‐mediated radiochemistry differs from fluorine‐18 and carbon‐11 approaches. In these cases, light facilitates a postlabeling click reaction, which has proven valuable for the labeling of large biomolecules such as monoclonal antibodies (mAbs). New technological developments, such as the incorporation of photoreactors in commercial radiosynthesizers, illustrate the commitment the field is making in embracing photochemistry. Taken together, these advances in photo‐mediated radiochemistry enable radiochemists to apply new retrosynthetic strategies in accessing novel PET radiotracers.