Scalable Approach to Fluorinated Heterocycles with Sulfur Tetrafluoride (SF4)

J. Org. Chem. 2021, 86 (17), 12181–12198

DOI: 10.1021/acs.joc.1c01518

Trofymchuk S.; Bugera M.; Klipkov A.; Ahunovych V.; Razhyk B.; Semenov S.; Boretskyi A.; Tarasenko K.; Mykhailiuk P.

A general approach to fluorinated (hetero)aromatic derivatives is elaborated. The key reaction is a deoxofluorination of substituted acetophenones with sulfur tetrafluoride (SF4). In contrast to previous deoxofluorination methods, this transformation is fast, scalable (up to 70 g), and high-yielding. More than 100 novel or previously hardly accessible fluorinated heterocycles, interesting for medicinal chemistry and agrochemistry, were synthesized.

Scalable Approach to Fluorinated Heterocycles with Sulfur Tetrafluoride (SF4)

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