Trifluoromethylation of alkyl electrophiles with ¹¹C- or ¹⁸F-labeled fluoroform for PET applications.

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 co

SUBMITTER: Wang C 

PROVIDER: S-EPMC12731722 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature