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Issue 4, 2019
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Direct construction of 2,3-unsubstituted benzofurans and benzothiophenes via a metal-free catalyzed intramolecular Friedel–Crafts reaction

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Abstract

A highly effective and straightforward method for the construction of 2,3-unsubstituted benzofurans and benzothiophenes by the intramolecular Friedel–Crafts reaction has been developed. This phosphoric acid-catalyzed method exhibits good functional group tolerance for both electron-withdrawing groups and electron-donating groups. We have successfully obtained benzofuran and benzothiophene derivatives with various substituents, and the yield was up to 94%. The development of this reaction provides a simple and efficient strategy for the construction of benzofuran and benzothiophene skeleton compounds.

Graphical abstract: Direct construction of 2,3-unsubstituted benzofurans and benzothiophenes via a metal-free catalyzed intramolecular Friedel–Crafts reaction

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Publication details

The article was received on 06 Nov 2018, accepted on 29 Dec 2018 and first published on 04 Jan 2019


Article type: Research Article
DOI: 10.1039/C8QO01204K
Org. Chem. Front., 2019,6, 493-497

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    Direct construction of 2,3-unsubstituted benzofurans and benzothiophenes via a metal-free catalyzed intramolecular Friedel–Crafts reaction

    W. Ma, J. Huang, X. Huang, S. Meng, Z. Yang, C. Li, Y. Wang, T. Qi and B. Li, Org. Chem. Front., 2019, 6, 493
    DOI: 10.1039/C8QO01204K

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