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一种基于浓度的用于氟亲核取代反应的微尺度方法及其在[F]FET和[F]氟哌利多一锅法放射性合成中的测试。

A concentration-based microscale method for F-nucleophilic substitutions and its testing on the one-pot radiosynthesis of [F]FET and [F]fallypride.

作者信息

Iwata Ren, Terasaki Kazunori, Ishikawa Yoichi, Harada Ryuichi, Furumoto Shozo, Yanai Kazuhiko, Pascali Claudio

机构信息

Cyclotron and Radioisotope Center, Tohoku University, Sendai, Japan.

Cyclotron Research Center, Iwate Medical University, Morioka, Japan.

出版信息

Appl Radiat Isot. 2020 Dec;166:109361. doi: 10.1016/j.apradiso.2020.109361. Epub 2020 Aug 3.

Abstract

When applied to a radiosynthesis, a microscale approach can help to save precursor and improve yields. Thus, a 5-10 μL microscale method based on a concentration procedure was developed and applied to the radiosynthesis of [F]FET and [F]fallypride. In spite of using an amount of precursor ca. 100 times smaller, radiochemical yields were comparable or even higher than those reported in literature. Because of the very low reaction volumes, the possible effects of concentrated dose of activity and carrier fluoride were also investigated.

摘要

当应用于放射性合成时,微尺度方法有助于节省前体并提高产率。因此,开发了一种基于浓缩程序的5-10μL微尺度方法,并将其应用于[F]FET和[F]氟哌利多的放射性合成。尽管使用的前体量约小100倍,但放射化学产率与文献报道的相当,甚至更高。由于反应体积非常小,还研究了活性和载体氟浓缩剂量的可能影响。

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