Copper-Catalyzed Enantioselective C-H Arylation between 2-Arylindoles and Hypervalent Iodine Reagents

The copper-catalyzed enantioselective C-H arylation between 2-arylindoles and hypervalent iodine reagents has been successfully developed, which provides a convenient and economical route to the highly atroposelective synthesis of axially chiral indole derivatives with a 2-aryl structure (up to 99% ee). Density functional theory calculations and wave function analysis show that the key sandwich intermediate leads to high enantioselectivity of the reaction.

Automated summary

The copper-catalyzed enantioselective C-H arylation between 2-arylindoles and hypervalent iodine reagents has been successfully developed, providing a convenient and economical route to the highly atroposelective synthesis of axially chiral indole derivatives with a 2-aryl structure (up to 99% ee). Computational analysis suggests that a key sandwich intermediate plays a crucial role in achieving high enantioselectivity in the reaction.