Collier Thomas Lee, Liang Steven H, Mann J John, Vasdev Neil, Kumar J S Dileep
Division of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Harvard Medical School, Boston, MA, USA.
Advion, Inc., Ithaca, NY, USA.
Beilstein J Org Chem. 2017 Dec 29;13:2922-2927. doi: 10.3762/bjoc.13.285. eCollection 2017.
Continuous-flow microfluidics has shown increased applications in radiochemistry over the last decade, particularly for both pre-clinical and clinical production of fluorine-18 labeled radiotracers. The main advantages of microfluidics are the reduction in reaction times and consumption of reagents that often result in increased radiochemical yields and rapid optimization of reaction parameters for F-labeling. In this paper, we report on the two-step microfluidic radiosynthesis of the high affinity partial agonist of the serotonin 1A receptor, [F]FEMPT (p = 9. 79; = 0.16 nM) by microfluidic radiochemistry. [F]FEMPT was obtained in ≈7% isolated radiochemical yield and in >98% radiochemical and chemical purity. The molar activity of the final product was determined to be >148 GBq/µmol (>4 Ci/µmol).
在过去十年中，连续流微流控技术在放射化学中的应用日益增加，特别是在氟 - 18标记放射性示踪剂的临床前和临床生产方面。微流控技术的主要优点是反应时间缩短和试剂消耗减少，这通常会提高放射化学产率，并能快速优化氟标记的反应参数。在本文中，我们报告了通过微流控放射化学两步法微流控放射合成血清素1A受体的高亲和力部分激动剂[F]FEMPT（p = 9.79； = 0.16 nM）。[F]FEMPT的分离放射化学产率约为7%，放射化学和化学纯度均>98%。最终产物的摩尔活度测定为>148 GBq/µmol（>4 Ci/µmol）。
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