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

J. Org. Chem. 2018, 83 (6), 3265-3274

DOI: 10.1021/acs.joc.8b00199

Levchenko V.; Dmytriv Y.; Tymtsunik A.; Liubchak K.; Rudnichenko A.; Melnyk A.; Veselovych S.; Borodulin Y.; Otsalyuk O.; Tolmachev A.; Mykhailiuk P.

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-1H-pyrazole, the known fungicide Penflufen, and many functionalized 5-fluoropyrazoles: building blocks for medicinal chemistry and agrochemistry.

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

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