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Updated: Jun 26, 2025

Enhancing Efficiency and Radiolabeling Yields of Carbon-11 Radioligands for Clinical Research Using the Loop Method
Published on: December 20, 2024
Radiodifluoromethylation of well-functionalized molecules
Wei Zhang1, Yinlong Li1, Steven H Liang1
1Department of Radiology and Imaging Sciences, Emory University Atlanta, Georgia 30322, USA.
Abstract:
The strategic installation of a [18F]fluorine atom at the specific position of the lead molecule is a never-ending challenge for radiochemists in their endeavour to develop novel positron emission tomography (PET) imaging applications. Although the radiosynthesis of [18F]CF2H-containing molecules has been explored in the past decade, more methods need to be explored for various well-functionalized compounds. Recently, two novel strategies of radiodifluoromethylation were reported, namely the utilization of [18F]difluorocarbene building block and frustrated Lewis pair-mediated C-18F bond formation, respectively. These methods provide an efficient radiofunctionalization of complex CF2H-containing molecules for drug discovery and PET ligand development.
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