Allylic Acetal as 3C Synthon in Rh(III)-Catalyzed Divergent C–H Activation/[4 + 3] Annulation: Easy Access to Benzodiazepines

A concise synthesis of benzodiazepines via Rh(III) catalyzed C-H activation/ [4 + 3] annulation of easily available 1-arylpyrazolidinones with allylic acetal has been developed. The allylic acetal was employed as a novel 3C synthon in this transformation. Benzodiazepines were built under mild reaction conditions with high efficiency and chemoselectivity. The high atom-economy and easily accessible substrates reveal potential application.

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Publication Details

Journal
Organic Letters
Published
2025-04-02
DOI
https://doi.org/10.1021/acs.orglett.4c04396
Citations
5
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
Field-Weighted Citation Impact
4.68

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article

Allylic Acetal as 3C Synthon in Rh(III)-Catalyzed Divergent C–H Activation/[4 + 3] Annulation: Easy Access to Benzodiazepines

Yangjie Wu, Xiuling Cui, Chao Pi, Mingming Hu
5 citations
Organic Letters
Catalytic C–H Functionalization Methods
4.68
article

Allylic Acetal as 3C Synthon in Rh(III)-Catalyzed Divergent C–H Activation/[4 + 3] Annulation: Easy Access to Benzodiazepines

Yangjie Wu, Xiuling Cui, Chao Pi, Mingming Hu
article en
5 citations

Abstract

A concise synthesis of benzodiazepines via Rh(III) catalyzed C-H activation/ [4 + 3] annulation of easily available 1-arylpyrazolidinones with allylic acetal has been developed. The allylic acetal was employed as a novel 3C synthon in this transformation. Benzodiazepines were built under mild reaction conditions with high efficiency and chemoselectivity. The high atom-economy and easily accessible substrates reveal potential application.

Organic LettersVol. 27(14)
Zhengzhou University (CN)
Science and Technology Department of Henan Province
Zero hunger
Openalex Percentile: Top 6%
Catalytic C–H Functionalization Methods
4.68
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Allylic Acetal as 3C Synthon in Rh(III)-Catalyzed Divergent C–H Activation/[4 + 3] Annulation: Easy Access to Benzodiazepines — Yangjie Wu, Xiuling Cui, et al. · Organic Letters (2025) | TGRS Research Map | TGRS