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无过渡金属碱催化2-炔基苯酚的分子内环化反应,用于高效便捷地合成2-取代苯并呋喃。

Transition-metal-free base catalyzed intramolecular cyclization of 2-ynylphenols for efficient and facile synthesis of 2-substituted benzo[]furans.

作者信息

Liu Yong, Lu Tao, Tang Wei-Fang, Gao Jian

机构信息

Department of Organic Chemistry, China Pharmaceutical University 24 Tong Jia Xiang Nanjing 210009 P. R. China

出版信息

RSC Adv. 2018 Aug 10;8(50):28637-28641. doi: 10.1039/c8ra03882a. eCollection 2018 Aug 7.

Abstract

A transition-metal-free base catalyzed intramolecular cyclization of 2-ynylphenols was developed for the facile synthesis of 2-substituted benzo[]furans. Various 2-aryl and 2-alkyl substituted benzo[]furans can be obtained with good to excellent yields using readily available CsCO as the catalyst under mild reaction conditions. The broad substrates scope and the typical maintenance of vigorous efficiency on gram scale make this protocol a potentially practical method to synthesize 2-substituted benzo[]furans derivatives.

摘要

开发了一种无过渡金属的碱催化2-炔基苯酚分子内环化反应,用于简便合成2-取代苯并呋喃。在温和的反应条件下,使用易于获得的碳酸铯作为催化剂,可以以良好至优异的产率获得各种2-芳基和2-烷基取代的苯并呋喃。广泛的底物范围以及在克级规模上典型的高效性使得该方法成为合成2-取代苯并呋喃衍生物的潜在实用方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b83/9084342/98a43c3b1a87/c8ra03882a-f1.jpg

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