Copper‐Catalyzed Radical Silylarylation of Activated Alkenes: Preparation of β‐Silyl Amide‐Pharmaceutical Hybrids

Abstract Copper‐catalyzed silylarylation of N ‐(arylsulfonyl)acrylamides via a tandem silyl radical addition/1,4‐aryl migration/desulfonylation sequence has been developed. This method employs silanes as the precursor of silyl radical and di‐ tert ‐butyl peroxide (DTBP) as the initiator. By using this cascade procedure, a series of β ‐silyl amide‐pharmaceutical hybrids which contain an α ‐all‐carbon quaternary stereocenter were facilely synthesized.