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Synthesis of Seven- and Eight-Membered Rings by a Brønsted Acid Catalyzed Cationic Carbocyclization of Biphenyl Embedded Enynes

Jaime Tostado, Ana Milián, Juan J. Vaquero, Manuel A. Fernández‐Rodríguez

2024Organic Letters11 citationsDOIOpen Access PDF

Abstract

High Resolution Image Download MS PowerPoint Slide A Brønsted acid catalyzed cyclization of o -alkenyl- o′ -alkynylbiaryls for the synthesis of biologically relevant dibenzo-fused medium-sized rings has been developed. The outcome of the cyclization is determined by the nature of the substituent at the alkyne, with arenes favoring seven-membered rings and alkyl substituents producing eight-membered rings. These reactions proceed via a vinyl cation, which is captured by water and, notably, by C-nucleophiles, such as electron-rich (hetero)arenes.

Topics & Concepts

ChemistryCationic polymerizationNucleophileSubstituentAlkyneBiphenylCatalysisBrønsted–Lowry acid–base theoryAlkylRing (chemistry)ElectrophileMedicinal chemistryStereochemistryOrganic chemistryCatalytic Alkyne ReactionsCatalytic C–H Functionalization MethodsCatalytic Cross-Coupling Reactions
Synthesis of Seven- and Eight-Membered Rings by a Brønsted Acid Catalyzed Cationic Carbocyclization of Biphenyl Embedded Enynes | Litcius