Acylative Coupling of Amine and Indole Using Chloroform as a Carbonyl Group
Acylative Coupling of Amine and Indole Using Chloroform as a Carbonyl Group
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DOI：
10.1002/ejoc.201800571
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发表时间：
2018-07
影响因子：
2.8
通讯作者：
Yui Nishida;Norihiko Takeda;K. Matsuno;O. Miyata;Masafumi Ueda
中科院分区：
文献类型：
--
作者：
Yui Nishida;Norihiko Takeda;K. Matsuno;O. Miyata;Masafumi Ueda
已经开发出氯仿介导的胺与吲哚的酰化偶联。当氯仿中的吲哚和胺在空气存在下用二甲基锌处理时，三组分氨基羰基化反应通过氯仿和O2原位生成光气进行，在一次操作中提供吲哚-3-甲酰胺。还描述了在生物活性化合物的合成和分子内酰化中的应用。
Chloroform‐mediated acylative coupling of amines with indoles has been developed. When indoles and amines in chloroform were treated with dimethylzinc in the presence of air, the three‐component aminocarbonylation reaction proceeded via in‐situ generation of phosgene from chloroform and O2to provide indole‐3‐carboxamides in a single operation. Application to the synthesis of biologically active compounds and intramolecular acylation are also described.