Expanding the Frontier of Linear Drug Design: Cu-Catalyzed Csp -Csp 3 -Coupling of Electron-Deficient SF4 -Alkynes with Alkyl Iodides.
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ABSTRACT: Despite the attractive properties of tetrafluorosulfanyl (SF4 ) compounds in drug discovery, medicinal research on SF4 molecules is hindered by the scarcity of suitable synthetic methodologies. Drawing inspiration from the well-established Sonogashira cross-coupling of terminal alkynes under Pd-catalysis, it is envisioned that SF4 -alkynes can serve as effective coupling partners. To overcome the challenges associated with the electron-deficient nature of SF4 -alkynes and the lability of the SF4 unit under transition-metal catalysis, an aryl radical mediated Csp -Csp 3 cross-coupling reaction is successfully developed under Cu catalysis. This methodology facilitates the coupling of SF4 -alkyn
SUBMITTER: Narra SR
PROVIDER: S-EPMC10953538 | biostudies-literature | 2024 Mar
REPOSITORIES: biostudies-literature
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