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• W4232963637 abstract "Molecules labeled with fluorine-18 are used as radiotracers for positron emission tomography. An important challenge is the labeling of arenes not amenable to aromatic nucleophilic substitution (SNAr) with [18F]F−. In the ideal case, the 18F fluorination of these substrates would be performed through reaction of [18F]KF with shelf-stable readily available precursors using a broadly applicable method suitable for automation. Herein, we describe the realization of these requirements with the production of 18F arenes from pinacol-derived aryl boronic esters (arylBPin) upon treatment with [18F]KF/K222 and [Cu(OTf)2(py)4] (OTf=trifluoromethanesulfonate, py=pyridine). This method tolerates electron-poor and electron-rich arenes and various functional groups, and allows access to 6-[18F]fluoro-L-DOPA, 6-[18F]fluoro-m-tyrosine, and the translocator protein (TSPO) PET ligand [18F]DAA1106." @default.
• W4232963637 created "2022-05-12" @default.
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• W4232963637 date "2014-06-10" @default.
• W4232963637 modified "2023-09-29" @default.
• W4232963637 title "A General Copper-Mediated Nucleophilic¹⁸F Fluorination of Arenes" @default.
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• W4232963637 doi "https://doi.org/10.1002/ange.201404436" @default.
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