American Chemical Society
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Scandium Triflate-Catalyzed N‑[18F]Fluoroalkylation of Aryl- Or Heteroaryl-Amines with [18F]Epifluorohydrin under Mild Conditions

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posted on 2022-05-25, 20:25 authored by Masayuki Fujinaga, Takayuki Ohkubo, Tomoteru Yamasaki, Katsushi Kumata, Nobuki Nengaki, Ming-Rong Zhang
The scandium triflate-catalyzed N-[18F]­fluoroalkylation of aryl- or heteroaryl-amines with [18F]­epifluorohydrin ([18F]2) was investigated. This reaction is mild and provides one-step access to N-[18F]­fluoroalkylated aryl- or heteroaryl-amines, which are used for positron emission tomography imaging. The use of 2,2,2-trifluoroethanol as a cosolvent improved the reaction efficiency. The use of (S)- and (R)-[18F]2 produced the corresponding enantiomeric N-[18F]­fluoroalkylated anilines.