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Azeotropic drying-free aliphatic radiofluorination to produce PET radiotracers in a mixed organic solvent system

Authors
 Young-Do Kwon  ;  Jeongmin Son  ;  Mijin Yun  ;  Joong-Hyun Chun 
Citation
 Tetrahedron Letters, Vol.59(29) : 2848-2852, 2018 
Journal Title
 Tetrahedron Letters 
ISSN
 0040-4039 
Issue Date
2018
Keywords
PET ; Fluorine-18 ; Radiofluorination ; PET radiotracer ; Automation
Abstract
Efficient aliphatic radiofluorination in a mixed organic solvent system was investigated. This method obviates the time-consuming [18F]fluoride drying step routinely required in the preparation of most fluorine-18 positron emission tomography (PET) radiotracers. The [18F]fluoride ions eluted from a QMA (quaternary ammonium anion exchange) cartridge with phase transfer agents were directly mixed in various organic solvents for subsequent radiofluorination. Herein, we report the azeotropic drying-free radiofluorination of aliphatic substrates and demonstrate the viability of hydrated [18F]fluoride ions in a mixed organic solvent system for obtaining useful radiochemical yields (RCYs). This practical and simple method has demonstrated general applicability to the production of established PET tracers as well as to the rapid assessment and chemical optimization of early-stage potential radiotracers.
Full Text
https://www.sciencedirect.com/science/article/pii/S0040403918307755
DOI
10.1016/j.tetlet.2018.06.033
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Nuclear Medicine (핵의학교실) > 1. Journal Papers
Yonsei Authors
Yun, Mi Jin(윤미진) ORCID logo https://orcid.org/0000-0002-1712-163X
Chun, Joong-Hyun(전중현) ORCID logo https://orcid.org/0000-0002-9665-7829
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URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/162636
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