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  • A New One-Pot Synthesis of ...
    Gabrielli, Serena; Giardinieri, Alessandra; Sampaolesi, Susanna; Ballini, Roberto; Palmieri, Alessandro

    Molecules (Basel, Switzerland), 06/2016, Letnik: 21, Številka: 6
    Journal Article

    Quinoline-2-carboxylates are an important subclass of quinoline derivatives largely present in a variety of biologically active molecules, as well as useful ligands in metal-catalyzed reactions. Herein, we present a new one-pot protocol for synthesizing this class of derivatives starting from β-nitroacrylates and 2-aminobenzaldehydes. In order to optimize the protocol, we investigated several reaction conditions, obtaining the best results using the 2-tert-Butylimino-2-diethylamino-1,3-dimethylperhydro-1,3,2-diazaphosphorine (BEMP) as solid base, in acetonitrile. Finally, we demonstrated the generality of our approach over several substrates which led to synthesize a plethora of functionalized quinolines-2-carboxylate derivatives in good overall yields.