title: Synthesis of 3-amino-4-fluoropyrazoles.
abstract: Fluorinated pyrazoles bearing additional functional groups that allow further functionalization are of considerable interest as building blocks in medicinal chemistry. The developed synthetic strategy for new 3-amino-4-fluoropyrazoles consists of a monofluorination of β-methylthio-β-enaminoketones using 1-(chloromethyl)-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (Selectfluor) toward the corresponding monofluorinated enaminoketones, followed by condensation with different hydrazines.
authors.affiliation: Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Gent, Belgium.
authors.forename: Riccardo
authors.initials: R
authors.lastname: Surmont
authors.forename: Guido
authors.initials: G
authors.lastname: Verniest
authors.forename: Mathias
authors.initials: M
authors.lastname: De Schrijver
authors.forename: Jan Willem
authors.initials: JW
authors.lastname: Thuring
authors.forename: Peter
authors.initials: P
authors.lastname: ten Holte
authors.forename: Frederik
authors.initials: F
authors.lastname: Deroose
authors.forename: Norbert
authors.initials: N
authors.lastname: De Kimpe
mesh_terms: D054879:Halogenation; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry*
chemical_list: D011720:Pyrazoles