Synthesis of γ-Carboline Derivatives via the Rh(III)-Catalyzed Regioselective C–H Activation/[4+2] Annulation Cascade

Transition-metal-catalyzed annulation represents an attractive approach for constructing diverse bioactive molecules while facing challenges like regioselective control. Herein, an efficient assembly of diverse highly functionalized γ-carboline derivatives from 2<i>H</i>-imidazoles and alkynes has been established. This was achieved through a rhodium(III)-catalyzed C-H activation/[4+2] tandem cyclization cascade, facilitating chemo- and regioselective access to γ-carbolines, which exhibit good anticancer activity, in moderate yields.

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Publication Details

Journal
Organic Letters
Published
2025-06-09
DOI
https://doi.org/10.1021/acs.orglett.5c01984
Citations
1
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
Field-Weighted Citation Impact
0.94

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article

Synthesis of γ-Carboline Derivatives via the Rh(III)-Catalyzed Regioselective C–H Activation/[4+2] Annulation Cascade

Yue Wei, Shenyou Nie, Yao Chen, Lijie Lv et al.
1 citations
Organic Letters
Catalytic C–H Functionalization Methods
0.94
article

Synthesis of γ-Carboline Derivatives via the Rh(III)-Catalyzed Regioselective C–H Activation/[4+2] Annulation Cascade

Yue Wei, Shenyou Nie, Yao Chen, Lijie Lv, Lida Wang, Yi He, Zhangshun Luo
article en
1 citations

Abstract

Transition-metal-catalyzed annulation represents an attractive approach for constructing diverse bioactive molecules while facing challenges like regioselective control. Herein, an efficient assembly of diverse highly functionalized γ-carboline derivatives from 2<i>H</i>-imidazoles and alkynes has been established. This was achieved through a rhodium(III)-catalyzed C-H activation/[4+2] tandem cyclization cascade, facilitating chemo- and regioselective access to γ-carbolines, which exhibit good anticancer activity, in moderate yields.

Organic LettersVol. 27(24)
Target (United States) (US), Chongqing Medical University (CN)
Chongqing Science and Technology Commission, Chongqing Municipal Education Commission, Venture and Innovation Support Program for Chongqing Overseas Returnees
Openalex Percentile: Top 25%
Catalytic C–H Functionalization Methods
0.94
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