Insight into the Axial Chirality in Benzodiazepines

1,4-Benzodiazepines, which are important core structures found in hypnotic and anxiolytic drugs, exhibit latent axial chirality. This article describes this axial chirality based on the sp2-sp2 axis arising from the Ar-NC(=O) axis (axis 1) and the Ar-C(=N) axis (axis 2). The dynamic axial chirality of this scaffold is considered a key core structure contributing to biological activity.

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Publication Details

Journal
Journal of Synthetic Organic Chemistry Japan
Published
2025-02-01
DOI
https://doi.org/10.5059/yukigoseikyokaishi.83.119
Primary Topic
Axial and Atropisomeric Chirality Synthesis
Type
article
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article

Insight into the Axial Chirality in Benzodiazepines

Hideaki Natsugari, Ryoko Tanaka, Hideyo Takahashi, Ryota Takano
Journal of Synthetic Organic Chemistry Japan
Axial and Atropisomeric Chirality Synthesis
article

Insight into the Axial Chirality in Benzodiazepines

Hideaki Natsugari, Ryoko Tanaka, Hideyo Takahashi, Ryota Takano
article en

Abstract

1,4-Benzodiazepines, which are important core structures found in hypnotic and anxiolytic drugs, exhibit latent axial chirality. This article describes this axial chirality based on the sp2-sp2 axis arising from the Ar-NC(=O) axis (axis 1) and the Ar-C(=N) axis (axis 2). The dynamic axial chirality of this scaffold is considered a key core structure contributing to biological activity.

Journal of Synthetic Organic Chemistry JapanVol. 83(2)
Tokyo University of Science (JP)
Zero hunger
Openalex Percentile: Top 98%
Axial and Atropisomeric Chirality Synthesis
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Insight into the Axial Chirality in Benzodiazepines — Hideaki Natsugari, Ryoko Tanaka, et al. · Journal of Synthetic Organic Chemistry Japan (2025) | TGRS Research Map | TGRS