Fluoro-functionalization is now recognized as a critical strategy in drug discovery; however, the accessible fluoro-functional groups are limited. We herein introduce an eccentric, fully fluorinated motif, -tetrafluoro-λ-sulfanyl -difluorocyclopropene . This novel motif is highly lipophilic and polarized, enabling a connection of two independent groups via three continuous atoms with a large angle of pseudo configuration. The target motif was synthesized via a [2+1] cycloaddition of electron-deficient (hetero)aryl-SF-alkynes with an electrophilic difluorocarbene source.
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http://dx.doi.org/10.1021/acs.orglett.2c00358 | DOI Listing |
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