Asymmetric Synthesis of Chiral Chromanes by Copper‐Catalyzed Hydroamination of 2 H ‐Chromenes

Hydroamination of Chromenes: A copper-catalyzed asymmetric hydroamination of 2H-chromenes employing hydrosilanes and hydroxylamine esters has been developed under mild reaction conditions. This strategy provides a straightforward approach to important chiral 4-aminochromanes and will widen the discovery of their unique bioactivity in medicinal chemistry.

A copper/(R)-DTBM-SEGPHOS-catalyzed enantioselective hydroamination of 2H-chromenes employing hydrosilanes and hydroxylamine esters has been developed. This protocol offers a highly efficient and direct route for accessing a series of 4-aminochromanes in 50–88 % yields with 59–99 % enantioselectivities under mild reaction conditions.