Copper-Catalyzed Dearomative Cyclopropanation of Benzofurans with Diynes via Vinyl Cations

Organic Letters 2026

View at publisher
Authors: Yan Xu, Yuan-Qing Dong, Jun Jiang, Cui‐Ting Li, Wei-Min He, Gongde Wu, Bo Zhou, Long‐Wu Ye
DOI: 10.1021/acs.orglett.5c05386
Cited by: 0
References: 58

Abstract

Dearomative cyclopropanation of benzofurans is a powerful strategy for the assembly of valuable O-heterocycles. However, transition metal-catalyzed cyclopropanation of benzofurans is generally limited to diazo compounds. Herein, a copper-catalyzed dearomative cyclopropanation of benzofurans with diynes via vinyl cations is described, enabling the atom-economical and practical synthesis of various cyclopropa[ b ]benzofurans in generally moderate to excellent yields. Furthermore, preliminary studies on asymmetric catalysis reveal that the desired chiral cyclopropa[ b ]benzofurans could be synthesized with good to excellent ee’s.

Fields of Study & Subjects

Cyclopropane Reaction Mechanisms Catalytic Alkyne Reactions Catalytic C–H Functionalization Methods

Publication details

Journal / source
Organic Letters
Volume
28
Issue
6
Pages
2090–2095
Publication date
3 February 2026
Language
EN