Acylative Coupling of Amine and Indole Using Chloroform as a Carbonyl Group

作者:Nishida Yuika; Takeda Norihiko; Matsuno Kenji; Miyata Okiko*; Ueda Masafumi*
来源:European Journal of Organic Chemistry, 2018, 2018(29): 3928-3935.
DOI:10.1002/ejoc.201800571

摘要

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 O-2 to provide indole-3-carboxamides in a single operation. Application to the synthesis of biologically active compounds and intramolecular acylation are also described.

  • 出版日期2018-8-7