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