The first synthesis of [11C]oseltamivir: a tool for elucidating the relationship between Tamiflu and its adverse effects on the central nervous system
✍ Scribed by Takuya Arai; Fujiko Konno; Masanao Ogawa; Ming-Rong Zhang; Kazutoshi Suzuki
- Publisher
- John Wiley and Sons
- Year
- 2009
- Tongue
- French
- Weight
- 411 KB
- Volume
- 52
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
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, ^11^C‐labeled oseltamivir was synthesized through a two‐step reaction involving [^11^C]acetylation with [1‐^11^C]acetyl chloride. Starting from approximately 37.0 GBq of [^11^C]CO~2~, 1.2–1.8 GBq (n=5) of [^11^C]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.