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

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.