Efficient Pd/AntPhos-catalyzed α-arylation of benzyl aryl ketones with aryl thianthrenium salts

Abstract

An efficient catalytic α-arylation of benzyl aryl ketones with aryl thianthrenium salts was developed using Pd/AntPhos as the catalyst. Various α-arylated benzyl phenyl ketones were produced with up to 98% yield. H₂O was necessary to achieve the high yields. This methodology was successfully applied to the efficient synthesis of droloxifene, tamoxifen and their analogs.