The first synthesis of [11C]oseltamivir: a tool for elucidating the relationship between Tamiflu and its adverse effects on the central nervous system

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. [11C]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.