Synthesis of Benzopyran Atropisomers via Electrophilic Halogenation

We report a halogenation‐based strategy for the synthesis of axially chiral benzopyrans, a rare and underexplored class of nonbiaryl atropisomers. The reaction exhibits broad substrate scope, tolerating both electron‐donating and electron‐withdrawing substituents, and accommodates the incorporation of bromine, chlorine, and iodine. A sequential double bromination enables the construction of bisbenzopyrans bearing two stereogenic axes. Preliminary enantioselective brominations catalyzed by chiral phosphoric acids delivered enantiomeric excesses of up to 56%. The method was successfully scaled to gram level and further elaborated through Suzuki coupling, highlighting its synthetic versatility. This work provides a new platform for the atroposelective synthesis of benzopyran‐based architectures.

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Publication Details

Journal
European Journal of Organic Chemistry
Published
2026-06-09
DOI
https://doi.org/10.1002/ejoc.70603
Primary Topic
Axial and Atropisomeric Chirality Synthesis
Type
article
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article

Synthesis of Benzopyran Atropisomers via Electrophilic Halogenation

Expédite Yen‐Pon, Damien Bonne, Alix Bourhis, Jean Rodriguez
European Journal of Organic Chemistry
Axial and Atropisomeric Chirality Synthesis
article

Synthesis of Benzopyran Atropisomers via Electrophilic Halogenation

Expédite Yen‐Pon, Damien Bonne, Alix Bourhis, Jean Rodriguez
article en

Abstract

We report a halogenation‐based strategy for the synthesis of axially chiral benzopyrans, a rare and underexplored class of nonbiaryl atropisomers. The reaction exhibits broad substrate scope, tolerating both electron‐donating and electron‐withdrawing substituents, and accommodates the incorporation of bromine, chlorine, and iodine. A sequential double bromination enables the construction of bisbenzopyrans bearing two stereogenic axes. Preliminary enantioselective brominations catalyzed by chiral phosphoric acids delivered enantiomeric excesses of up to 56%. The method was successfully scaled to gram level and further elaborated through Suzuki coupling, highlighting its synthetic versatility. This work provides a new platform for the atroposelective synthesis of benzopyran‐based architectures.

European Journal of Organic Chemistry
Centre National de la Recherche Scientifique (FR), Centrale Méditerranée (FR)
Openalex Percentile: Top 12%
Axial and Atropisomeric Chirality Synthesis
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