Copper-catalyzed remote sulfonylation of alkynyl naphthalene esters with aromatic sodium sulfinates.

Sulfones serve as key scaffolds in bioactive molecules and drugs, and aromatic-spaced alkynyl sulfones are difficult to synthesize owing to alkyne assembly and remote activation limitations. A novel copper-catalyzed remote sulfonylation is established to construct such compounds using alkynyl naphthalene esters and aromatic sulfinates. Wide substrate generality and favorable functional group tolerance are demonstrated. Gram-scale synthesis and structural derivatization are conducted, which offer an efficient strategy and expand the scope of remote alkyne functionalization.