Palladium‐Catalyzed Domino Heck/Phosphorylation towards 3,3‐Disubstituted Phosphinonyloxindoles

The first Pd‐catalyzed domino Heck/phosphorylation of N‐(2‐iodophenyl)acrylamides with secondary phosphine oxides has been developed. The use of PdCl2 as a catalyst, 1,4‐bis(diphenylphosphino)butane as a ligand, K2CO3 as a base, various N‐(2‐iodophenyl)acrylamide derivatives are tolerant in this transformation, affording 3‐phosphinomethyl 3,3‐disubstituted oxindole products in good to excellent yields. This transformation offers a straightforward route to the formation of the new C−C and P−C bonds, oxindole ring in one step. Moreover, this method can be easily adapted to large‐scale preparation.