Catalyst-free three-component synthesis of highly functionalized 2,3-dihydropyrroles
Résumé
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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Catalyst-Free Three-Component Synthesis of 23-Dihydropyrroles_sans marque.pdf (1.3 Mo)
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