一种用于有机化合物电化学氟 - 氟化反应的自动化合成器。
An automated synthesizer for electrochemical F-fluorination of organic compounds.
作者信息
Waldmann Christopher M, Lebedev Artem, Allison Nathaniel, Sadeghi Saman
机构信息
Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, University of California Los Angeles, 650 Charles E Young Dr. S, Los Angeles, CA 90095, United States.
出版信息
Appl Radiat Isot. 2017 Sep;127:245-252. doi: 10.1016/j.apradiso.2017.06.028. Epub 2017 Jun 21.
Abstract
Electrochemical F-fluorination of organic compounds provides a means to synthesize Positron-Emission-Tomography (PET) tracers difficult to obtain otherwise. Here, the first automated synthesizer that enables radiolabeling through carrier-added electrochemical F-fluorination is described. The system provides capabilities for all necessary operations such as drying of cyclotron derived [F]fluoride, electrochemical incorporation of the radioisotope into a precursor molecule, subsequent reactions such as protecting group removals, HPLC-purification and formulation of the final tracer. Demonstrated is the aliphatic electrochemical F-fluorination of methyl 2-(phenylthio)acetate.
摘要
有机化合物的电化学F-氟化提供了一种合成正电子发射断层扫描（PET）示踪剂的方法，否则这些示踪剂很难获得。本文描述了第一台能够通过添加载体的电化学F-氟化进行放射性标记的自动化合成仪。该系统具备所有必要操作的能力，如回旋加速器衍生的[F]氟化物的干燥、放射性同位素向前体分子的电化学掺入、后续反应（如保护基团去除）、HPLC纯化以及最终示踪剂的配制。展示了2-（苯硫基）乙酸甲酯的脂肪族电化学F-氟化反应。
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