Preparation of 5-Fluoropyrazoles from Pyrazoles and N-Fluorobenzenesulfonimide (NFSI)

Facile synthesis of 5-fluoropyrazoles by direct fluorination of pyrazoles with N-fluorobenzenesulfonimide (NFSI) was elaborated. This approach was used to prepare the unsubstituted 5-fluoro-1 H-pyrazole, the known fungicide Penflufen, and many functionalized 5-fluoropyrazoles: building blocks for me...

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Veröffentlicht in:Journal of organic chemistry 2018-03, Vol.83 (6), p.3265-3274
Hauptverfasser: Levchenko, Vitalina, Dmytriv, Yurii V, Tymtsunik, Andriy V, Liubchak, Konstantin, Rudnichenko, Alexander, Melnyk, Anton V, Veselovych, Stanislav Y, Borodulin, Yurii V, Otsalyuk, Oleksandr M, Tolmachev, Andrei A, Mykhailiuk, Pavel K
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Sprache:eng
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Zusammenfassung:Facile synthesis of 5-fluoropyrazoles by direct fluorination of pyrazoles with N-fluorobenzenesulfonimide (NFSI) was elaborated. This approach was used to prepare the unsubstituted 5-fluoro-1 H-pyrazole, the known fungicide Penflufen, and many functionalized 5-fluoropyrazoles: building blocks for medicinal chemistry and agrochemistry.
ISSN:0022-3263
1520-6904
DOI:10.1021/acs.joc.8b00199