Radiosynthesis of O-[11C]methyl-L-tyrosine and O-[18F]fluoromethyl-L-tyrosine as potential PET tracers for imaging amino acid transport
Radiosynthesis of O-[11C]methyl-L-tyrosine and O-[18F]fluoromethyl-L-tyrosine as potential PET tracers for imaging amino acid transport
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DOI：
10.1002/jlcr.696
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发表时间：
2003-05-01
影响因子：
1.8
通讯作者：
Ishiwata, K
中科院分区：
文献类型：
--
作者：
Iwata, R;Furumoto, S;Ishiwata, K
制备了两种酪氨酸的正电子发射类似物O-[C-11]甲基-L-酪氨酸和O-[F-18]氟甲基-L-酪氨酸作为新型肿瘤显像剂。在室温下将烷基化剂[C-11]三氟甲磺酸甲酯或[F-18]三氟甲磺酸甲酯氟简单地鼓泡通过L-酪氨酸二钠盐的二甲亚砜溶液。经过随后的 HPLC 纯化，基于相应的标记剂，获得了标记的 L-酪氨酸类似物，经衰变校正的放射化学收率超过 50%，放射化学纯度始终高于 98%。相当简单的制备过程以及所实现的高放射化学产率，使得这两种合成方法都适合常规生产。版权所有 (C) 2003 John Wiley Sons, Ltd.
Two positron-emitting analogues of tyrosine, O-[C-11]methyl-L-tyrosine and O-[F-18]fluoromethyl-L-tyrosine were prepared as new tumor imaging agents. The alkylating agent, [C-11]methyl triflate or [F-18]fluoromethyl triflate, was simply bubbled through a dimethylsulfoxide solution Of L-tyrosine disodium salt at room temperature. After subsequent HPLC purification the labeled L-tyrosine analogues were obtained in decay-corrected radiochemical yields of over 50%, based on their corresponding labeling agent, with radiochemical purities always higher than 98%. The quite straightforward preparation, together with the high radiochemical yields achieved, make both these syntheses suitable for routine production. Copyright (C) 2003 John Wiley Sons, Ltd.