Catalyst-Controlled Switchable Mono-/Di-C–H Arylation of Aromatic Amides with Arylsilanes

The selective mono/di-C-H arylation of aromatic amides has been developed, enabling efficient coupling with arylsilanes under mild conditions with good functional group tolerance. The regioselectivity (mono- vs diarylation) is catalyst-dependent, with [Cp*RhCl<sub>2</sub>]<sub>2</sub> selectively promoting monoarylation, whereas [Cp*IrCl<sub>2</sub>]<sub>2</sub> demonstrates a distinct preference for diarylation. This approach establishes a straightforward and efficient strategy for the late-stage arylation of pharmaceutical compounds.

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Publication Details

Journal
Organic Letters
Published
2025-09-20
DOI
https://doi.org/10.1021/acs.orglett.5c03239
Citations
1
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
Field-Weighted Citation Impact
0.94
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article

Catalyst-Controlled Switchable Mono-/Di-C–H Arylation of Aromatic Amides with Arylsilanes

Yi Dong, Tingting Hou, Wenwu Liu, Heng Xu et al.
1 citations
Organic Letters
Catalytic C–H Functionalization Methods
0.94
article

Catalyst-Controlled Switchable Mono-/Di-C–H Arylation of Aromatic Amides with Arylsilanes

Yi Dong, Tingting Hou, Wenwu Liu, Heng Xu, Ming‐Chun Lu, Xin Yang, Deyu Wu, Mengmeng Li
article en
1 citations

Abstract

The selective mono/di-C-H arylation of aromatic amides has been developed, enabling efficient coupling with arylsilanes under mild conditions with good functional group tolerance. The regioselectivity (mono- vs diarylation) is catalyst-dependent, with [Cp*RhCl<sub>2</sub>]<sub>2</sub> selectively promoting monoarylation, whereas [Cp*IrCl<sub>2</sub>]<sub>2</sub> demonstrates a distinct preference for diarylation. This approach establishes a straightforward and efficient strategy for the late-stage arylation of pharmaceutical compounds.

Organic LettersVol. 27(39)
Guiyang Medical University (CN), Chinese Academy of Medical Sciences & Peking Union Medical College (CN), Peking University (CN), Peking Union Medical College Hospital (CN), Shanghai Institute of Materia Medica (CN), Peking University First Hospital (CN), Institute of Medicinal Plant Development (CN)
Openalex Percentile: Top 21%
Catalytic C–H Functionalization Methods
0.94
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