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. 2018 Dec 7;20(23):7699-7702.
doi: 10.1021/acs.orglett.8b03429. Epub 2018 Nov 13.

Brønsted Acid Mediated Cascade Reaction To Access 3-(2-Bromoethyl)benzofurans

Stefania Porcu  1 , Stefania Demuro  1 , Alberto Luridiana  1 , Andrea Cocco  1 , Angelo Frongia  1 , David J Aitken  2 , Florence Charnay-Pouget  2 , Regis Guillot  2 , Giorgia Sarais  3 , Francesco Secci  1
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Brønsted Acid Mediated Cascade Reaction To Access 3-(2-Bromoethyl)benzofurans

Stefania Porcu et al. Org Lett. .

Abstract

A unified protocol for the construction of 3-(2-bromoethyl)benzofurans and 2-(benzofuran-3-yl)ethylamines from bis[(trimethylsilyl)oxy]cyclobutene has been developed. This mild and facile strategy was applied for the synthesis of a series of 5-HT serotonin receptor agonists, underlining its potential for the syntheses of bioactive compounds and natural products.

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