Copper‐Catalyzed Ring Opening of Benzofurans and an Enantioselective Hydroamination Cascade

Abstract

Abstract A copper(II) acetate/( R )‐DTBM‐SEGPHOS‐catalyzed ring opening of benzofurans and enantioselective hydroamination cascade with dimethoxymethylsilane (DMMS) and hydroxylamine esters is described. Starting from readily available substituted benzofurans, a series of chiral N,N‐dibenzylaminophenols, which are of high interest in pharmaceutical chemistry, were obtained with excellent enantioselectivities (up to 66 % yield, 94 % ee ).