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首页> 外文期刊>EJNMMI Radiopharmacy and Chemistry >A new approach to produce [18F]MC225 via one-step synthesis, a PET radiotracer for measuring P-gp function
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A new approach to produce [18F]MC225 via one-step synthesis, a PET radiotracer for measuring P-gp function

机译：通过一步合成生产[18F] MC225的新方法，用于测量P-GP功能的宠物放射反射器

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Background[ 18 F]MC225 is a radiotracer for imaging P-glycoprotein (P-gp) function at the blood-brain barrier. The P-gp function can be altered due to different factors, for instance, decreased P-gp function has been described in patients with Alzheimer’s or Parkinson’s Disease. The current applied radiosynthesis of [ 18 F]MC225 involves 2 steps, including the distillation of the [ 18 F] fluoroethylbromide intermediate. To develop a more robust synthetic procedure, it is of interest to produce the radiotracer via a 1-step synthesis. The present study describes a new synthetic approach to produce [ 18 F]MC225 via direct 18 F-fluorination. Moreover, we also provide the appropriate conditions for the automation of the synthesis. A mesylate precursor was synthesized via a multi-step synthetic route and used for the radiolabeling. The nucleophilic substitution of the mesylate group by [ 18 F] Fluoride was automated in two different synthesis modules: IBA Synthera and Eckert and Ziegler PharmTracer (E&Z).ResultsThe mesylate precursor was synthesized in 7 steps starting with 5-hydroxy-1-tetralone (commercially available) in practical yields. The stability of the precursor was improved via mesylate salt formation method. The radiolabeling was done by adding the mesylate precursor dissolved in DMF to the dried [ 18 F]KF/K 2.2.2 complex and heating at 140?°C for 30?min. Quality control by UPLC confirmed the production of [ 18 F]MC225 with a molar activity (A m ) higher than 100?GBq/micromole. The synthesis time in Synthera was 106?min and the product was obtained with a radiochemical purity higher than 95% and RCY of 6.5%, while the production in E&Z lasted 120?min and the product had a lower radiochemical purity (91%) and RCY (3.8%).Conclusions[ 18 F]MC225 was successfully produced via a 1-step reaction. The procedure is suitable for automation using commercially available synthesis modules. The automation of the radiosynthesis in the Synthera module allows the production of the [ 18 F]MC225 by a reliable and simple method.
机译：背景技术MC225是用于在血脑屏障处成像的p-糖蛋白（P-GP）功能的放射反射液。例如，由于不同的因素，可以改变P-GP功能，例如，在阿尔茨海默氏症或帕金森病的患者中描述了降低的P-GP功能。 [18 f] MC225的电流施加的覆盖合成涉及2步，包括[18 f]氟乙基溴体中间体的蒸馏。为了开发更稳健的合成程序，通过1步合成产生放射性机构是有意义的。本研究描述了一种新的合成方法，通过直接18 F氟化产生[18 f] MC225。此外，我们还为合成的自动化提供了适当的条件。通过多步合成途径合成甲磺酸盐前体并用于放射性标记。氟化甲酸盐基团的亲核取代氟化物在两个不同的合成模块中自动化：IBA Synthera和Eckert和Ziegler Pharmtracer（E＆Z）。甲磺酸酯前体在7个步骤中合成，以5-羟基-1-Tetralone（以实际收益率市售）。通过甲磺酸盐形成方法改善了前体的稳定性。通过将溶解在DMF中的甲磺酸盐前体加入干燥的[18 f] Kf / K 2.2.2复合物并在140℃下加热30℃，通过加热30≤min。 UPLC的质量控制证实了[18 F] MC225的产生，其摩尔活性（A M）高于100？GBQ / microOle。同联的合成时间为106〜min，并将产物的放射化学纯度高于95％，Rcy为6.5％，而E＆Z的产量持续120℃，产品较低的放射化学纯度（91％）和RCY（3.8％）。结论通过1步反应成功生产[18f] MC225。该过程适用于使用市售的合成模块的自动化。在Synthera模块中的可放射合成的自动化允许通过可靠且简单的方法生产[18 F] MC225。

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