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Issue 12, 2018
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Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles

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Abstract

An efficient synthesis of fully substituted 2,3-dihydropyrroles has been achieved in one step through the three-component reaction of amines, aromatic aldehydes and α-ketoamides. This atom-economical and catalyst-free reaction is highly stereoselective and generates underexplored heterocycles in a single step. These compounds were examined in an enzymatic assay that led to the identification of potent α-glucosidase inhibitors, thereby demonstrating the utility of this novel methodology in medicinal chemistry.

Graphical abstract: Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles

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Publication details

The article was received on 28 Mar 2018, accepted on 13 May 2018 and first published on 23 May 2018


Article type: Paper
DOI: 10.1039/C8GC00987B
Citation: Green Chem., 2018,20, 2775-2780
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    Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles

    D. Wang, L. Li, H. Feng, H. Sun, F. Almeida-Veloso, M. Charavin, P. Yu and L. Désaubry, Green Chem., 2018, 20, 2775
    DOI: 10.1039/C8GC00987B

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