Volume 136, Issue 14 e202317136
Aufsatz

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

Daniel Lin

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

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Dr. Laura M. Lechermann

Dr. Laura M. Lechermann

Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA

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Malcolm P. Huestis

Malcolm P. Huestis

Discovery Chemistry, Genentech, Inc., DNA Way, South San Francisco, CA 94080 USA

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Dr. Jan Marik

Dr. 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

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Dr. Jeroen B. I. Sap

Corresponding Author

Dr. Jeroen B. I. Sap

Department of Translational Imaging, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080 USA

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First published: 22 December 2023
Citations: 1

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 [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.

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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