Extending the substrate scope of palladium-catalyzed arylfluorination of allylic amine derivatives

JOURNAL OF FLUORINE CHEMISTRY(2024)

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摘要
Fluorinated molecules often show superior bioactivity or ADME (absorption, distribution, metabolism, and excretion) properties compared to their non-fluorinated analogues. In fact, 20-30 % of newly approved drugs and the majority of recently approved agrochemicals are organofluorine compounds. Unsurprisingly, there is great interest in the development of new and/or improved processes for fluorine incorporation. Pd-catalyzed arylfluorination of alkenes is a novel, emerging fluorination method, which simultaneously introduces a fluorine atom and an aryl group into an alkene framework. The aim of the current work was studying, improving, and extending a literature arylfluorination protocol, which originally utilized N-allylated sulfonamide substrates.
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关键词
Alkenes,Arylation,Arylfluorination,Fluorination,Olefin difunctionalization,Palladium catalysis
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