Improved synthesis of [11C]SA4503, [11C]MPDX and [11C]TMSX by use of [11C]methyl triflate
Improved synthesis of [11C]SA4503, [11C]MPDX and [11C]TMSX by use of [11C]methyl triflate
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使用 [11C] 三氟甲磺酸甲酯改进 [11C]SA4503、[11C]MPDX 和 [11C]TMSX 的合成
DOI：
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发表时间：
2004
影响因子：
2.6
通讯作者：
K. Ishiwata
中科院分区：
文献类型：
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作者：
K. Kawamura;K. Ishiwata
最近，我们在临床上使用了三个新的放射性配基，[11C]SA4503，[11C]MPDX和[11C]TSMX，分别用于通过正电子发射断层扫描来定位人脑中的Sigmai、腺苷A1和腺苷A2a受体。这些放射性配体是通过各自的去甲基前体与[11C]甲基碘甲基化而合成的。在这里，我们通过使用[11C]三氟酸甲酯改进了这些化合物的合成，这是一种高活性的[11C]碘甲烷替代品。
Recently we have clinically used three new radioligands, [11C]SA4503, [11C]MPDX, and [11C]TMSX, for mapping sigmai, adenosine A1, and adenosine A2A receptors, respectively, in the human brain by positron emission tomography. These radioligands are synthesized by methylation of the respective demethyl precursor with [11C]methyl iodide. Here we demonstrate the improved syntheses of these compounds by use of [11C]methyl triflate, a highly reactive alternative to [11C]methyl iodide.