What question did this study set out to answer?

To develop a mild rhodium(III)-catalyzed direct C2-alkylation of indoles using cyclopropanols and demonstrate its application in synthesizing complex indole-fused heterocycles.

August 16, 2026The Journal of Organic Chemistry

Rhodium(III)-CatalyzedDirect C–H Alkylationof Indoles with Cyclopropanols and Its Application in the DivergentSynthesis of Indole-Fused Seven-Membered Heterocycles

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Authors

RLRuilian LiangGuangzhou University HCHuanlin ChenGuangzhou University CSChengyang SongGuangzhou University

Discussion

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Overview

Experimental study demonstrates rhodium-catalyzed C2-alkylation of indoles with cyclopropanols, enabling concise synthesis of indole-fused seven-membered heterocycles.

Key Points

To develop a mild rhodium(III)-catalyzed direct C2-alkylation of indoles using cyclopropanols and demonstrate its application in synthesizing complex indole-fused heterocycles.
Coupled various indoles with cyclopropanols via Rh(III)-catalyzed oxidative C–H activation under mild reaction conditions.
Subjected the resulting carbonyl-containing N-carboxamide indole products to concise two-step derivatizations to form fused ring scaffolds.
Successfully generated an array of β-indolyl ketones with broad functional group compatibility under mild conditions.
Achieved divergent synthesis of two distinct classes of indole-fused seven-membered heterocycles through straightforward two-step transformations.

Cite This Study

Liang et al. (2026) studied this question.

synapsesocial.com/papers/6a817a33f2fb91fc834ade11 https://doi.org/10.1021/acs.joc.6c01441

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August 16, 2026The Journal of Organic Chemistry

Rhodium(III)-CatalyzedDirect C–H Alkylationof Indoles with Cyclopropanols and Its Application in the DivergentSynthesis of Indole-Fused Seven-Membered Heterocycles

View Full Paper

Ask AI

Bookmark

Authors

RLRuilian LiangGuangzhou University HCHuanlin ChenGuangzhou University CSChengyang SongGuangzhou University

Discussion

Member takes

Overview

Experimental study demonstrates rhodium-catalyzed C2-alkylation of indoles with cyclopropanols, enabling concise synthesis of indole-fused seven-membered heterocycles.

Key Points

To develop a mild rhodium(III)-catalyzed direct C2-alkylation of indoles using cyclopropanols and demonstrate its application in synthesizing complex indole-fused heterocycles.
Coupled various indoles with cyclopropanols via Rh(III)-catalyzed oxidative C–H activation under mild reaction conditions.
Subjected the resulting carbonyl-containing N-carboxamide indole products to concise two-step derivatizations to form fused ring scaffolds.
Successfully generated an array of β-indolyl ketones with broad functional group compatibility under mild conditions.
Achieved divergent synthesis of two distinct classes of indole-fused seven-membered heterocycles through straightforward two-step transformations.

Cite This Study

Liang et al. (2026) studied this question.

synapsesocial.com/papers/6a817a33f2fb91fc834ade11 https://doi.org/10.1021/acs.joc.6c01441

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