Radiosynthesis of 18F-fluoroethylated tracers via a simplified one-pot 18F-fluoroethylation method using [18F]fluoroethyl tosylate

Kazunori Kawamura; Katsushi Kumata; Wakana Mori; Masayuki Fujinaga; Yusuke Kurihara; Masanao Ogawa; Takayuki Ohkubo; Kenji Furutsuka; Hiroki Hashimoto; Nobuki Nengaki; Ming-Rong Zhang

doi:10.1016/j.apradiso.2020.109571

Radiosynthesis of ¹⁸F-fluoroethylated tracers via a simplified one-pot ¹⁸F-fluoroethylation method using [¹⁸F]fluoroethyl tosylate

Appl Radiat Isot. 2021 Mar:169:109571. doi: 10.1016/j.apradiso.2020.109571. Epub 2020 Dec 26.

Affiliations

¹ Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-855, Japan. Electronic address: kawamura.kazunori@qst.go.jp.
² Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-855, Japan.
³ Department of Advanced Nuclear Medicine Sciences, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba, 263-855, Japan; SHI Accelerator Service Ltd., Tokyo, 141-0032, Japan.

PMID: 33412382
DOI: 10.1016/j.apradiso.2020.109571

Abstract

Recently, a straightforward one-pot method for ¹⁸F-fluoroethylation without azeotropic drying of cyclotron-produced [¹⁸F]F^- was developed. In this study, we have attempted to simplify the automated radiosynthesis of two [¹⁸F]fluoroethylated tracers, [¹⁸F]FEDAC and [¹⁸F]FET, using a desmethyl labeling precursor and [¹⁸F]fluoroethyl tosylate, based on the above-mentioned method. The radiochemical yields of [¹⁸F]FEDAC and [¹⁸F]FET were 26 ± 3.7% (n = 5) and 14 ± 2.2% (n = 4), respectively, based on total [¹⁸F]F^- at the end of irradiation.

Keywords: (18)F-fluoroethylation; One-pot; [(18)F]FEDAC; [(18)F]FET; [(18)F]fluoroethyl tosylate.