A new convenient method for the synthesis of [2-C]thymine utilizing [C]phosgene |
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| Authors: | Kazue Ohkura Ken-ichi Nishijima Yuji Kuge Koh-ichi Seki |
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| Affiliation: | a Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido, Ishikari-Tobetsu, Hokkaido 061-0293, Japan
b Graduate School of Medicine, Hokkaido University, Kita-15, Nishi-7, Kita-ku, Sapporo 060-8638, Japan |
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| Abstract: | β-(N-Benzoylamino)methacrylamide, a key intermediate for the preparation of [2-11C]thymine, was synthesized in three steps from ethyl α-formylpropionate and NH3. Reaction of the alkali metal salts of β-(N-benzoylamino)methacrylamide with [11C]phosgene gave [2-11C]thymine. The yield of [2-11C]thymine was 362 ± 53 MBq at EOS (n = 3) (18 MeV proton beam; 10 μA, 10 min). The total synthesis was accomplished in just 16 min from the end of bombardment. |
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| Keywords: | EOS, end of synthesis EOB, end of bombardment PET, positron emission tomography DME, 1,2-dimethoxyethane |
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