Abstract
A sustainable and atom economic one-pot synthesis of biologically significant 3-hydroxy-2-pyrrolidone moieties via the reaction of benzyl amine, aniline (or another benzyl amine) and dialkylacetylenedicarboxylate without catalyst in green solvent has been developed. Some remarkable features of our green procedure are aqueous ethanol solvent, reaction without catalyst, no column chromatography for isolation of the products, higher the value of atom economy (AE) (up to 94.30 %) and lower the E-factor value (up to 0.23 g/g). The reaction principally demonstrates the scope of oxidation of benzyl amines followed by cyclization. This synthetic route is also applicable to gram-scale synthesis.
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