Light-Driven Radiochemistry with Fluorine-18, Carbon-11 and Zirconium-89
Daniel Lin
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Current address: University of Southern California Department of Chemistry, Loker Hydrocarbon Research Institute, 837 Bloom Walk, Los Angeles, CA 90089 USA
Search for more papers by this authorDr. Laura M. Lechermann
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorMalcolm P. Huestis
Discovery Chemistry, Genentech, Inc., DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorDr. Jan Marik
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Discovery Chemistry, Genentech, Inc., DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorCorresponding Author
Dr. Jeroen B. I. Sap
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorDaniel Lin
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Current address: University of Southern California Department of Chemistry, Loker Hydrocarbon Research Institute, 837 Bloom Walk, Los Angeles, CA 90089 USA
Search for more papers by this authorDr. Laura M. Lechermann
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorMalcolm P. Huestis
Discovery Chemistry, Genentech, Inc., DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorDr. Jan Marik
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Discovery Chemistry, Genentech, Inc., DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorCorresponding Author
Dr. Jeroen B. I. Sap
Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA
Search for more papers by this authorAbstract
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 [18F]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 11C-methylation, 11C-carboxylation, 11C-carbonylation, and 11C-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.
Conflict of interests
The authors declare no conflict of interest.
Open Research
Data Availability Statement
Data sharing is not applicable to this article as no new data were created or analyzed in this study.
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