2025-12-18 バージニア工科大学(Virginia Tech)
A high resolution PET CT scan of the human brain. Photo courtesy of Adobe Stock.
<関連情報>
- https://news.vt.edu/articles/2025/12/science-chemistry-wliu-pet-tracer.html
- https://www.science.org/doi/10.1126/science.ady2969
PET用途のための11Cまたは18 F標識フルオロホルムによるアルキル求電子剤のトリフルオロメチル化 Trifluoromethylation of alkyl electrophiles with 11C- or 18F-labeled fluoroform for PET applications
Chao Wang, Paul DeMent, Susovan Jana, Jinsoo Hong, […] , and Wei Liu
Science Published:18 Dec 2025
DOI:https://doi.org/10.1126/science.ady2969
Editor’s summary
Positron emission tomography (PET) requires the use of tracers labeled with radioactive isotopes, most commonly fluorine-18 or carbon-11. Because these isotopes begin to decay immediately upon generation, it is advantageous to incorporate them into the tracer framework in a small number of simple steps. Wang et al. report a versatile method to introduce either label to alkyl groups in a wide variety of molecules using a copper-catalyzed reaction of fluoroform. The protocol relies on activation of the alkyl center either through iodine abstraction by an aryl radical or photoredox-induced decarboxylation. —Jake S. Yeston
Abstract
Continued development of positron emission tomography (PET) tracers is essential for advancing molecular imaging in biomedical research and clinical diagnostics. A long-standing limitation in radiochemistry for PET imaging has been the lack of general methods for radiolabeling trifluoromethyl (CF3) groups at C(sp3) sites, despite their growing prevalence in bioactive molecules and radiopharmaceuticals. Here, we present a general approach for late-stage installation of either a [18F]CF3 or [11C]CF3 group at a C(sp3) site. This method leverages unusual copper-mediated radiotrifluoromethylation of alkyl halides and alkyl carboxylic acids by halogen atom transfer and photoredox catalysis, respectively. More than 50 complex molecules and pharmaceutical agents were efficiently labeled with fluorine-18 (18F) or carbon-11 (11C). Two long-sought-after radioligands, [18F]SL25.1188 and [18F]PS13, were synthesized, providing longer-lived 18F analogs of their 11C counterparts with great promise for human PET imaging.
