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

Novák, Tamás T. and Nguyen, Chi Cam Tu and Gömöry, Ágnes and Hornyánszky, Gábor and Remete, Attila Márió and Kiss, Loránd (2024) Extending the substrate scope of palladium-catalyzed arylfluorination of allylic amine derivatives. JOURNAL OF FLUORINE CHEMISTRY, 273. No-110239. ISSN 0022-1139

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Abstract

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 fluo- rine 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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