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Diversity-oriented synthesis of benzofuro[3,2-<i>b</i>]pyridine derivatives from aurone-derived α,β-unsaturated imines and activated terminal alkynes

Bin Cheng, Hui Li, Xuecheng Zhu, Xinping Zhang, Yixuan He, Haiyan Sun, Taimin Wang, Hongbin Zhai

2021Chemical Communications19 citationsDOI

Abstract

An efficient annulation reaction of aurone-derived α,β-unsaturated imines and activated terminal alkynes mediated by triethylamine is described, which enables the facile synthesis of 1,4-dihydrobenzofuro[3,2-b]pyridines in high yields. When the nucleophile of triethylamine was replaced with triphenylphosphine, another class of 1,4-dihydrobenzofuro[3,2-b]pyridines tethered with an additional acrylate motif were obtained instead. These two types of 1,4-dihydrobenzofuro[3,2-b]pyridines could be aromatized in the presence of DBU to afford benzofuro[3,2-b]pyridines, which could also be accessed via a one-pot procedure.

Topics & Concepts

Terminal (telecommunication)ChemistryCatalysisPyridineMedicinal chemistryStereochemistryOrganic chemistryComputer scienceTelecommunicationsCatalytic C–H Functionalization MethodsSynthesis of Organic CompoundsSynthesis and Reactivity of Heterocycles
Diversity-oriented synthesis of benzofuro[3,2-<i>b</i>]pyridine derivatives from aurone-derived α,β-unsaturated imines and activated terminal alkynes | Litcius