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

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

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.

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