Fully automated synthesis and purification of 4‐(2′‐methoxyphenyl)‐1‐[2′‐(N‐2″‐pyridinyl)‐p‐[18F]fluorobenzamido]ethylpiperazine |
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| Authors: | Kazutaka Hayashi Kenji Furutsuka Takehito Ito Masatoshi Muto Hatsumi Aki Toshimitsu Fukumura Kazutoshi Suzuki |
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| Institution: | 1. Radiopharmaceutical Production Team, Molecular Probe Group, Molecular Imaging Center, National Institute of Radiological Sciences (NIRS), , Chiba, 263‐8555 Japan;2. Molecular Imaging Integration Unit, RIKEN Center for Molecular Imaging Science (CMIS), , Hyogo, 650‐0047 Japan;3. SHI Accelerator Service Co., Ltd., , Tokyo, 141‐0032 Japan;4. Tokyo Nuclear Service Co., Ltd., , Tokyo, 110‐0016 Japan;5. Department of Pharmaceuticals, Faculty of Pharmaceutical Sciences, Fukuoka University, , Fukuoka, 814‐80 Japan |
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| Abstract: | We have developed an efficient synthesis method for the rapid and high‐yield automated synthesis of 4‐(2′‐methoxyphenyl)‐1‐2′‐(N‐2″‐pyridinyl)‐p‐18F]fluorobenzamido]ethylpiperazine (p‐18F]MPPF). No‐carrier‐added 18F]F? was trapped on a small QMA cartridge and eluted with 70% MeCN(aq) (0.4 mL) containing Kryptofix 222 (2.3 mg) and K2CO3 (0.7 mg). The nucleophilic 18F]fluorination was performed with 3 mg of the nitro‐precursor in DMSO (0.4 mL) at 190 °C for 20 min, followed by the preparative HPLC purification (column: COSMOSIL Cholester, Nacalai Tesque, Kyoto, Japan; mobile phase: MeCN/25 mm AcONH4/AcOH = 200/300/0.15; flow rate: 6.0 mL/min) to afford p‐18F]MPPF (retention time = 9.5 min). p‐18F]MPPF was obtained automatically with a radiochemical yield of 38.6 ± 5.0% (decay corrected, n = 5), a specific activity of 214.3 ± 21.1 GBq/µmol, and a radiochemical purity of >99% within a total synthesis time of about 55 min. Copyright © 2012 John Wiley & Sons, Ltd. |
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| Keywords: | 5‐HT1A receptor p‐[18F]MPPF [18F]fluoride automated synthesis preparative HPLC separation |
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