Design and Applications of a SO₂ Surrogate in Palladium‐Catalyzed Direct Aminosulfonylation between Aryl Iodides and Amines

Abstract

A new SO₂ surrogate is reported that is cheap, bench-stable, and can be accessed in just two steps from bulk chemicals. Essentially complete SO₂ release is achieved in 5 minutes. Eight established sulfonylation reactions proceeded smoothly by ex situ formation of SO₂ by utilizing a two-chamber system in combination with the SO₂ surrogate. Furthermore, we report the first direct aminosulfonylation between aryl iodides and amines. Broad functional group tolerance is demonstrated, and the method is applicable to pharmaceutically relevant substrates, including heterocyclic substrates.