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Copper-Catalyzed Aza-Michael Addition of 2‑Aminobenzoate to β‑Substituted α,β-Unsaturated Ketones: One-Pot Synthesis of 3‑Carbonyl-2-Substituted Quinolin-4(1H)‑ones

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journal contribution
posted on 09.02.2018, 15:41 by Seongil Kang, Subin Park, Kyung-su Kim, Changsik Song, Yunmi Lee
We present a new and straightforward one-pot process for the synthesis of 3-carbonyl-4-quinolone derivatives through highly efficient Cu-catalyzed aza-Michael addition of 2-aminobenzoates to β-substituted α,β-unsaturated ketones/cyclization/mild oxidation reactions. A broad range of new versatile 3-carbonyl-quinolin-4­(1H)-ones is prepared from readily available chemicals under mild reaction conditions with short reaction times, producing good to excellent yields (up to 99%).