Copper-mediated 77Br, 125I, and 211At radiohalogenation of aryl thianthrenium salts using visible light
This article describes a Cu-mediated visible-light ipso-radiohalogenation of thianthrenium salts with bromine-77, iodine-125 and astatine-211. Thianthrenium precursors provide late-stage, regioselective access to labelled (hetero)arenes, delivering radiohalides in moderate to high radiochemical yields within 1 min at room temperature. Notably, radioastatination proceeds without photocatalysts, revealing distinct photoreactivity. The optimised protocols were applied to functionally dense small molecules, including a methoxyestrone derivative featuring a steroidal template common in many radiopharmaceuticals.
Authors
- Shelbie Jaylene Cingoranelli (ORCID: https://orcid.org/0009-0002-5578-0342)
- Paul Martorano (ORCID: https://orcid.org/0000-0001-8824-0065)
- Surendra Reddy Gundam
- Robert H. Mach (ORCID: https://orcid.org/0000-0002-7645-2869)
- Paul A. Ellison (ORCID: https://orcid.org/0000-0002-8379-7419)
- Peter J. H. Scott (ORCID: https://orcid.org/0000-0002-6505-0450)
- Eric Webb (ORCID: https://orcid.org/0000-0003-1501-9022)
- Gregory D. Bowden (ORCID: https://orcid.org/0000-0003-2274-6738)
- Casey J. McCarthy (ORCID: https://orcid.org/0000-0002-3967-5705)
- Jay Samuel Wright (ORCID: https://orcid.org/0000-0002-1350-123X)
- Mehran Makvandi (ORCID: https://orcid.org/0000-0002-6315-4942)
- Hsiaoju S. Lee (ORCID: https://orcid.org/0000-0001-9082-8618)
- Hong Beom Lee
- Siran Qian
- Kevin Cheng
Institutions
- University of Wisconsin–Madison (US)
- University of Michigan (US)
- University of Wisconsin Health (US)
- University of Pennsylvania (US)
Publication Details
- Journal
- npj Imaging
- Published
- 2026-09-29
- DOI
- https://doi.org/10.1038/s44303-026-00194-3
- Primary Topic
- Chemical Reactions and Isotopes
- Type
- article
- Field-Weighted Citation Impact
- 0.00