Atroposelective remote meta-C−H arylation of 2-arylanilines

Abstract

Enantioselective remote C−H activation is a challenging task in organic chemistry, and atroposelective synthesis of remotely substituted axially chiral molecules via direct C−H activation remains elusive. In this issue of Chem, Yu, Wang, and co-workers report an atroposelective meta-C−H arylation of 2-arylanilines via an enantioselective palladation relay strategy. Enantioselective remote C−H activation is a challenging task in organic chemistry, and atroposelective synthesis of remotely substituted axially chiral molecules via direct C−H activation remains elusive. In this issue of Chem, Yu, Wang, and co-workers report an atroposelective meta-C−H arylation of 2-arylanilines via an enantioselective palladation relay strategy. Atroposelective remote meta-C–H activationLi et al.ChemMay 1, 2023In BriefThe stereoselective and expedient preparation of axially chiral compounds, abundant in chiral catalysts, pharmaceuticals, and natural products, is a critical objective in synthesis. More specifically, accessing remotely substituted axially chiral motifs remains a significant challenge. We disclose an atroposelective Pd-catalyzed remote C–H activation arylation of 2-arylanilines via an enantioselective palladation relay strategy. This protocol enables direct access to valuable new axially chiral chemical space. Full-Text PDF