TY - JOUR T1 - Iodonium Ylide–Mediated Radiofluorination of <sup>18</sup>F-FPEB and Validation for Human Use JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 489 LP - 492 DO - 10.2967/jnumed.114.151332 VL - 56 IS - 3 AU - Nickeisha A. Stephenson AU - Jason P. Holland AU - Alina Kassenbrock AU - Daniel L. Yokell AU - Eli Livni AU - Steven H. Liang AU - Neil Vasdev Y1 - 2015/03/01 UR - http://jnm.snmjournals.org/content/56/3/489.abstract N2 - Translation of new methodologies for labeling nonactivated aromatic molecules with 18F remains a challenge. Here, we report a one-step, regioselective, metal-free 18F-labeling method that uses a hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical 18F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile (18F-FPEB). Methods: Automated radiosynthesis of 18F-FPEB was achieved by reaction of the ylide precursor (4 mg) with 18F-Et4NF in dimethylformamide at 80°C for 5 min and formulated for injection within 1 h. Results: 18F-FPEB was synthesized in 20% ± 5% (n = 3) uncorrected radiochemical yields relative to 18F-fluoride, with specific activities of 666 ± 51.8 GBq (18 ± 1.4 Ci)/μmol at the end of synthesis and was validated for human use. Conclusion: Radiofluorination of iodonium (III) ylides proved to be an efficient radiosynthetic strategy for synthesis of 18F-labeled radiopharmaceuticals. ER -