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

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 in a single step underexplored heterocycles. 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.
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Green Chemistry, Royal Society of Chemistry, 2018, 20 (12), pp.2775-2780. 〈10.1039/C8GC00987B〉
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Dong Wang, Linna Li, Hairong Feng, Hua Sun, Fabrice Almeida-Veloso, et al.. Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles. Green Chemistry, Royal Society of Chemistry, 2018, 20 (12), pp.2775-2780. 〈10.1039/C8GC00987B〉. 〈hal-01829592〉

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