The first synthesis of [11C]oseltamivir: a tool for elucidating the relationship between Tamiflu and its adverse effects on the central nervous system |
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| Authors: | Takuya Arai Fujiko Konno Masanao Ogawa Ming‐Rong Zhang Kazutoshi Suzuki |
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| Institution: | 1. Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences, 4‐9‐1 Anagawa, Inage‐ku, Chiba 263‐8555, Japan;2. SHI Accelerator Service Co. Ltd., 1‐17‐6 Osaki, Shinagawa‐ku, Tokyo 141‐8686, Japan |
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| Abstract: | Oseltamivir phosphate (Tamiflu ® ) is an anti‐influenza drug approved in many countries. Recently, in Japan, adverse effects on the central nervous system have been reported in younger patients administrated with Tamiflu. As a tool for elucidating the relationship between Tamiflu and its adverse effects, 11C‐labeled oseltamivir was synthesized through a two‐step reaction involving 11C]acetylation with 1‐11C]acetyl chloride. Starting from approximately 37.0 GBq of 11C]CO2, 1.2–1.8 GBq (n=5) of 11C]oseltamivir was obtained at the end of synthesis (EOS) 36–39 min after the end of bombardment. Radiochemical purity and specific activity were greater than 98% and 2.7–6.3 GBq/µmol at EOS, respectively. Copyright © 2009 John Wiley & Sons, Ltd. |
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| Keywords: | [11C]oseltamivir [1‐11C]acetyl chloride PET |
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