A concentration-based microscale method for 18F-nucleophilic substitutions and its testing on the one-pot radiosynthesis of [18F]FET and [18F]fallypride

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

doi:10.1016/j.apradiso.2020.109361

A concentration-based microscale method for ¹⁸F-nucleophilic substitutions and its testing on the one-pot radiosynthesis of [¹⁸F]FET and [¹⁸F]fallypride

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

Authors

Ren Iwata¹, Kazunori Terasaki², Yoichi Ishikawa¹, Ryuichi Harada³, Shozo Furumoto¹, Kazuhiko Yanai³, Claudio Pascali⁴

Affiliations

¹ Cyclotron and Radioisotope Center, Tohoku University, Sendai, Japan.
² Cyclotron Research Center, Iwate Medical University, Morioka, Japan.
³ Graduate School of Medicine, Tohoku University, Sendai, Japan.
⁴ Fondazione IRCCS Istituto Nazionale dei Tumori, V. Venezian, 1, Milan, 20133, Italy. Electronic address: [email protected].

PMID: 32877862
DOI: 10.1016/j.apradiso.2020.109361

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 [¹⁸F]FET and [¹⁸F]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.

Keywords: Concentration by evaporation; Microscale reaction; [(18)F]FET; [(18)F]fallypride.