Synthesis of 2,2,5-Trisubstituted Tetrahydrofurans by Ferrocenium-Catalyzed Dehydrative Diol Cyclization Reactions

A ferrocenium-catalyzed synthesis of trisubstituted tetrahydrofurans by dehydrative cyclization of diols is reported. Treatment of γ-phenyl-γ-butyrolactone or valerolactone with 2–3 equivalents of MeLi, <i>n</i>-BuLi, or PhLi yielded the corresponding substituted 1,4-butanediols in 41–86...

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Bibliographic Details
Main Authors: Cody D. Amann, Khushboo, Eike B. Bauer
Format: Article
Language:English
Published: MDPI AG 2025-02-01
Series:Inorganics
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Online Access:https://www.mdpi.com/2304-6740/13/2/59
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Summary:A ferrocenium-catalyzed synthesis of trisubstituted tetrahydrofurans by dehydrative cyclization of diols is reported. Treatment of γ-phenyl-γ-butyrolactone or valerolactone with 2–3 equivalents of MeLi, <i>n</i>-BuLi, or PhLi yielded the corresponding substituted 1,4-butanediols in 41–86% yields. Subsequent dehydrative cyclization of the diols under non-inert conditions using catalytic ferrocenium tetrafluoroborate (10 mol%) produced trisubstituted tetrahydrofurans in 72–83% yields after 48–72 h at 45–70 °C in CH<sub>2</sub>Cl<sub>2</sub>. This study demonstrates ferrocenium-catalyzed dehydrative cyclization for the first time, offering a convenient route to substituted tetrahydrofurans in two steps from commercial or easily accessible starting materials.
ISSN:2304-6740