Broad-scope Syntheses of [¹¹ C/¹⁸ F]Trifluoromethylarenes from Aryl(mesityl)iodonium Salts.

ABSTRACT: Efficient methods for labeling aryl trifluoromethyl groups to provide novel radiotracers for use in biomedical research with positron emission tomography (PET) are keenly sought. We report a broad-scope method for labeling trifluoromethylarenes with either carbon-11 (t_1/2 =20.4 min) or fluorine-18 (t_1/2 =109.8 min) from readily accessible aryl(mesityl)iodonium salts. In this method, the aryl(mesityl)iodonium salt is treated rapidly with no-carrier-added [¹¹ C]CuCF₃ or [¹⁸ F]CuCF₃ . The mesityl group acts as a spectator allowing radiolabeled trifluoromethylarenes to be obtained with very high chemoselectivity. Radiochemical yields from aryl(mesityl)iodonium salts bearing either electron-donating or electron-withdrawing groups

SUBMITTER: Telu S 

PROVIDER: S-EPMC10192059 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature