Copper‐Mediated Aminoquinoline‐Directed Radiofluorination of Aromatic C−H Bonds with K18F.

A Cu‐mediated ortho‐C−H radiofluorination of aromatic carboxylic acids that are protected as 8‐aminoquinoline benzamides is described. The method uses K18F and is compatible with a wide range of functional groups. The reaction is showcased in the high specific activity automated synthesis of the RARβ2 agonist [18F]AC261066. Late‐stage fluorination: K18F is applied in a newly developed Cu‐mediated ortho‐C(sp2)−H radiofluorination of aromatic carboxylic acids that are protected as 8‐aminoquinoline benzamides. Fluorination of 18 examples in up to 62 % radiochemical yield and high specific activity is reported, including the automated synthesis of [18F]AC261066. [ABSTRACT FROM AUTHOR]