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Updated: Jun 5, 2025

18F-Labeling of Radiotracers Functionalized with a Silicon Fluoride Acceptor SiFA for Positron Emission Tomography
Published on: January 11, 2020
Late-Stage Rapid [18F]Trifluoromethyl Radiolabeling of Terminal Alkenes at Room Temperature
Xuefei Li1,2, Lang Xie3, Shun Huang4
1Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education, School of Pharmacy, Zunyi Medical University, Zunyi 563003, China.
Abstract:
We report an efficient, metal-free method for late-stage rapid [18F]trifluoromethyl radiolabeling of terminal alkenes at room temperature. Utilizing 3,3-difluoroallyl sulfonium salts as precursors, the process achieves high radiochemical yields (up to 94 ± 2%) in just 30 s, with excellent functional group tolerance. This method offers a simplified and efficient pathway to produce [18F]trifluoromethylated terminal alkene compounds, enabling their application in PET imaging and expanding the chemical space for drug discovery.
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