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

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. H<sub>2</sub>O was necessary to achieve the high yields. This methodology was successfully applied to the efficient synthesis of droloxifene, tamoxifen and their analogs.

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Publication Details

Journal
Chemical Communications
Published
2025-12-02
DOI
https://doi.org/10.1039/d5cc06260h
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

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

Rui Shi, Guodu Liu, Xiangdong Zhang
Chemical Communications
Catalytic C–H Functionalization Methods
article

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

Rui Shi, Guodu Liu, Xiangdong Zhang
article en

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. H<sub>2</sub>O was necessary to achieve the high yields. This methodology was successfully applied to the efficient synthesis of droloxifene, tamoxifen and their analogs.

Chemical CommunicationsVol. 62(5)
Mongolian Academy of Sciences (MN), Inner Mongolia University (CN), Inner Mongolia Academy of Agricultural & Animal Husbandry Sciences (CN), Inner Mongolia University of Technology (CN)
Openalex Percentile: Top 71%
Catalytic C–H Functionalization Methods
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