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Updated: Mar 19, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
A New One-Pot Synthesis of Quinoline-2-carboxylates under Heterogeneous Conditions
Serena Gabrielli1, Alessandra Giardinieri2, Susanna Sampaolesi3
1Green Chemistry Group, Chemistry Division, School of Science and Technology, University of Camerino, via S. Agostino 1, 62032 Camerino, Italy. serena.gabrielli@unicam.it.
Abstract:
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.
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