Radiochemistry and Biomarker Development Unit, Department of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, Vienna 1090, Austria.
Bioorg Med Chem. 2012 Oct 1;20(19):5936-40. doi: 10.1016/j.bmc.2012.07.051. Epub 2012 Aug 7.
Changes in the expression of the melanin concentrating hormone receptor 1 (MCHR1) are involved in a variety of pathologies, especially obesity and anxiety disorders. To monitor these pathologies in-vivo positron emission tomography (PET) is a suitable method. After the successful radiosynthesis of [(11)C]SNAP-7941-the first PET-Tracer for the MCHR1, we aimed to synthesize its [(18)F]fluoroethylated analogue: [(18)F]FE@SNAP. Therefore, microfluidic and vessel-based approaches were tested. [(18)F]fluoroethylation was conducted via various [(18)F]fluoroalkylated synthons and direct [(18)F]fluorination. Only the direct [(18)F]fluorination of a tosylated precursor using a flow-through microreactor was successful, affording [(18)F]FE@SNAP in 44.3 ± 2.6%.
黑色素浓缩激素受体 1(MCHR1)表达的变化与多种病理学有关,特别是肥胖和焦虑症。正电子发射断层扫描(PET)是监测这些病理学的合适方法。在成功合成 [(11)C]SNAP-7941(第一个用于 MCHR1 的 PET 示踪剂)后,我们旨在合成其 [(18)F] 氟乙基类似物:[(18)F]FE@SNAP。因此,我们测试了微流控和基于容器的方法。通过各种 [(18)F] 氟烷基化合成子和直接 [(18)F] 氟化进行 [(18)F] 氟乙基化。只有使用流通式微反应器对 tosylated 前体进行直接 [(18)F] 氟化才成功,得到 [(18)F]FE@SNAP 的产率为 44.3±2.6%。