Waldmann Christopher M, Lebedev Artem, Allison Nathaniel, Sadeghi Saman
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.
Appl Radiat Isot. 2017 Sep;127:245-252. doi: 10.1016/j.apradiso.2017.06.028. Epub 2017 Jun 21.
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.
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。
