One-step synthesis of 4-[(18) F]fluorobenzyltriphenylphosphonium cation for imaging with positron emission tomography.

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