Department of Chemistry, Kwangwoon University , Seoul 01897, Republic of Korea.
Department of Chemistry, Sungkyunkwan University , Suwon 16419, Republic of Korea.
J Org Chem. 2018 Mar 2;83(5):2694-2705. doi: 10.1021/acs.joc.7b03162. Epub 2018 Feb 9.
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%).
我们提出了一种新的、简便的一锅法合成 3-羰基-4-喹啉酮衍生物的方法，该方法通过高效的 Cu 催化 2-氨基苯甲酸酯与β-取代的α,β-不饱和酮的氮杂迈克尔加成/环化/温和氧化反应实现。通过温和的反应条件和短的反应时间，从易得的化学物质出发，制备了广泛的新型多功能 3-羰基-4(1H)-喹啉酮，产率良好至优秀（高达 99%）。
