Preparation method of beta-aminoketone

The invention discloses a preparation method of beta-aminoketone. According to the preparation method, aromatic ring substituted propargyl alcohol and amide are taken as raw materials, and tandem Meyer-Schuster rearrangement reaction and intermolecular amine hydrogenation addition reaction are perfo...

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Bibliographische Detailangaben
Hauptverfasser: DUAN YONGBIN, SUN YUE, ZHANG HUA, SUN YUXING, YIN YAN, TAO RUIHENG, WEI HUAZHENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of beta-aminoketone. According to the preparation method, aromatic ring substituted propargyl alcohol and amide are taken as raw materials, and tandem Meyer-Schuster rearrangement reaction and intermolecular amine hydrogenation addition reaction are performed by the action of acid, so that one-pot synthesis of beta-aminoketone is achieved. The maximum output of the preparation method of beta-aminoketone can reach 94%; the method has the advantages of simplicity in operation, 100% atom use ratio, economy and the like; and a novel synthesis method is provided for constructing beta-aminoketone compounds. 本发明公开了种β-氨基酮的制备方法。该制备方法以芳环取代的丙炔醇和酰胺为原料,在酸作用下进行串联的Meyer-Schuster重排反应和分子间胺氢化加成反应,从而实现β-氨基酮的锅法合成。本发明的β-氨基酮的制备方法最高产率可达94%,具有操作简单和100%原子经济等优点,为β-氨基酮类化合物的构建提供了种全新的合成方法。