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One‐step synthesis of 4‐[ 18 F]fluorobenzyltriphenylphosphonium cation for imaging with positron emission tomography
Author(s) -
Zhang Zhengxing,
Zhang Chengcheng,
Lau Joseph,
Colpo Nadine,
Bénard François,
Lin KuoShyan
Publication year - 2016
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3436
Subject(s) - chemistry , trifluoromethanesulfonate , phosphonium , positron emission tomography , counterion , radiochemistry , copper , pet imaging , combinatorial chemistry , ion , nuclear medicine , organic chemistry , catalysis , medicine
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.