The tetrafluoro-λ-sulfanyl (SF) moiety has been relatively undeveloped since its discovery in the 1970s. In this study, we synthesized pyridine-SF-isoxazolines, in which the two heterocycles are connected by a rodlike -SF linker, via the regioselective 1,3-dipolar cycloaddition of pyridine-SF-alkynes and nitrones in the presence of triethylamine. SF linkers are a viable alternative to para-substituted benzenes, alkynes, and bicyclo[1.1.1]pentyl derivatives in drug design, and pyridine-SF-isoxazolines have potential applications in drug development.
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