A palladium-catalyzed α-arylation reaction of unactivated sulfones with aryl chlorides is presented. High reactivity and chemoselectivity was achieved with a combination of Buchwald's 2nd generation palladium precatalyst and Kwong's indole-based phosphine… Click to show full abstract
A palladium-catalyzed α-arylation reaction of unactivated sulfones with aryl chlorides is presented. High reactivity and chemoselectivity was achieved with a combination of Buchwald's 2nd generation palladium precatalyst and Kwong's indole-based phosphine ligand. A variety of aryl chlorides and aryl methyl sulfones were coupled in good to excellent yields. A gram-scale arylation was also successfully conducted. Chemoselective arylation of the sulfone was observed over Buchwald–Hartwig amination.
               
Click one of the above tabs to view related content.