Aβ斑块显像剂:11C-PIB的合成及标记

    Synthesis and Carbon Labeling of 11C-PIB for Aβ-Amyloid Imaging

    • 摘要: 11C标记2(4′-N-11C-甲胺基苯)-6-羟基苯并噻唑(6-OH-BTA-1)是目前较理想的Aβ斑块显像剂,本研究合成了6-OH-BTA-1的前体:6-羟基-2-(4′-氨基苯基)苯并噻唑,并用11C标记。在常温下,无需保护羟基条件下,标记效率为52.6%(校正,n=35),产品放射化学纯度大于99%,比活度为18.0 TBq/mmol。80℃加热2 min,有副反应发生。采用弱酸性流动相,半制备HPLC分离后产品的放射化学纯度达99%。

       

      Abstract: Assessing the deposition of Aβ-amyloid in the living brain is important for diagnosis and treatment of Alzheimer’s disease(AD). 2-(4′-N-11C-methyl-aminophenyl)-6-hydroxybenzothiazole( 11C-PIB) was used as a ideal labeled probe imaging Aβ-amyloid for AD. The precursor of 11C-PIB, 2-(4′-aminophenyl)-6-hydroxybenzothiazole, was synthesized. 11C-PIB was labeled with 11C-CH3-Triflate(Trifluoromethanesulfonate)under unprotect 6-hydroxyl precursor at room temperature. The labeling yield, radiochemistry purity and specific activity are 52.6%(corrected, n=35), 99% and 18.0TBq/mmoL respectively. The by reaction occurrs when the reaction is heated 80℃ for 2 min. The radiochemistry purity can be improved to 99% by semi-HPLC weak acid mobile phase.

       

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