Syntheses of Acridones via Copper(II)-Mediated Relay Reactions from o-Aminoacetophenones and Arylboronic Acids
Syntheses of Acridones via Copper(II)-Mediated Relay Reactions from o-Aminoacetophenones and Arylboronic Acids
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通过铜(II)介导的邻氨基苯乙酮和芳基硼酸的中继反应合成吖啶酮
DOI：
10.1021/acs.orglett.8b00957
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发表时间：
2018-05-18
期刊：
影响因子：
5.2
通讯作者：
Zhang, Guisheng
中科院分区：
文献类型：
--
作者：
Wu, Hao;Zhang, Zhiguo;Zhang, Guisheng
邻氨基苯乙酮和芳基硼酸的反应，在吡啶的存在下，在O-2气氛下，铜（II）盐催化提供了一个通用的和有效的一锅制备生物有趣的吖啶酮。该中继反应包括分子间Suzuki交叉偶联、分子内氧化C（sp（3））-H胺化和C（sp（2））-H活化，同时重排生成的靛红中间体。该策略容许供电子和吸电子官能团两者，以良好至优异的产率提供各种吖啶酮。
The reaction of o-aminoacetophenones and arylboronic acids catalyzed by copper(II) salts in the presence of pyridine under an O-2 atmosphere provides a general and efficient one-pot preparation of biologically interesting acridones. This relay reaction comprises an intermolecular Suzuki cross-coupling, intramolecular oxidative C(sp(3))-H amination, and C(sp(2))-H activation with simultaneous rearrangement of the generated isatin intermediates. This strategy tolerates both electron-donating and -withdrawing functionalities to afford various acridones in good to excellent yields.