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Scalable Approach to Fluorinated Heterocycles with Sulfur Tetrafluoride (SF4)
Serhii Trofymchuk1,2, Maksym Bugera1,3, Anton A Klipkov1,3
1Enamine Ltd., Chervonotkatska 78, 02094 Kyiv, Ukraine.
Abstract:
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.
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