量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum and Radiological Science and Technology.
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The nitroaldol reaction of nitro[11C]methane and formaldehyde, which yields 2-(hydroxymethyl)-2-nitro[2-11C]propane-1,3-diol, is explored. The fluoride-ion-assisted nitroaldol reaction using (C4H9)4NF was rapid and provided the desired nitrotriol in more than 97% radiochemical conversion (decay-corrected) in 3 min at room temperature. Neither 2-nitro[2-11C]ethanol nor 2-nitro[2-11C]propane-1,3-diol was observed under the reaction conditions. The preparation of 2-amino-2-(hydroxymethyl)-[2-11C]propane-1,3-diol ([11C]Tris) was described, which was followed by the nitro-group reduction using NiCl2 and NaBH4 in aqueous MeOH. The decay-corrected radiochemical conversion to [11C]Tris was 68.0+/-6.5% in two steps.
雑誌名
Journal of Labelled Compounds & Radiopharmaceuticals
Nitroaldol reaction of nitro[11C]methane to form 2-(hydroxymethyl)-2-nitro[2-11C]-propane-1,3-diol and [11C]Tris
