Improved synthesis of anti-[18F]FACBC:: improved preparation of labeling precursor and automated radiosynthesis
Improved synthesis of anti-[18F]FACBC:: improved preparation of labeling precursor and automated radiosynthesis
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DOI：
10.1016/s0969-8043(03)00029-0
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发表时间：
2003-06-01
影响因子：
1.6
通讯作者：
Goodman, MM
中科院分区：
文献类型：
--
作者：
McConathy, J;Voll, RJ;Goodman, MM
非天然氨基酸抗1-氨基-3-[F-18]氟环丁基-1-羧酸（FACBC）已显示出正电子发射断层扫描肿瘤成像的前景。设计了一种改进的抗[F-18]FACBC前体的合成方法，该方法具有高的立体选择性，适合于大规模制备。已经开发了一种自动放射合成，其以24%的衰变校正产率提供抗[F-18]FACBC。此外，抗[F-18]FACBC剂量中存在的主要非放射性物质已被鉴定为抗1-氨基-3-羟基环丁烷-1-羧酸。总之，这些结果是朝着常规生产人用抗[F-18]FACBC迈出的重要一步。(C)2003爱思唯尔科技有限公司版权所有。
The non-natural amino acid anti-1-amino-3-[F-18]fluorocyclobutyl-1-carboxylic acid (FACBC) has shown promise for tumor imaging with positron emission tomography. An improved synthesis of the precursor of anti-[F-18]FACBC has been devised which demonstrates high stereoselectivity and suitability for large-scale preparations. An automated radiosynthesis has been developed which provides anti-[F-18]FACBC in 24% decay-corrected yield. Additionally, the major non-radioactive species present in doses of anti-[F-18]FACBC has been identified as anti-1-amino-3-hydroxycyclobutane-1-carboxylic acid. Together, these results are important steps towards the routine production of anti-[F-18]FACBC for human use. (C) 2003 Elsevier Science Ltd. All rights reserved.