One‐step synthesis of 4‐[18F]fluorobenzyltriphenylphosphonium cation for imaging with positron emission tomography

4‐[¹⁸F]Fluorobenzyltriphenylphosphonium cation (¹⁸F‐FBnTP) is a promising negative membrane potential targeting positron emission tomography tracer. However, the reported multistep radiolabeling approach for the synthesis of ¹⁸F‐FBnTP poses a challenge for routine clinical applications. In this study, we demonstrated that ¹⁸F‐FBnTP can be prepared in good conversion yields (~60%, nondecay corrected) in just one step via a copper‐mediated ¹⁸F‐fluorination reaction using a pinacolyl arylboronate precursor. In addition, our data suggest that ¹⁸F‐labeled (phosphonium) cations can be efficiently prepared via a copper‐mediated ¹⁸F‐fluoronation by using triflate as the counterion.