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钯催化吲哚与卤代炔烃的区域选择性 C-H 炔基化反应:合成官能化的 7-炔基吲哚。

Palladium-catalyzed regioselective C-H alkynylation of indoles with haloalkynes: access to functionalized 7-alkynylindoles.

机构信息

Key Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510640, China.

State Key Laboratory of Luminescent Materials and Devices, South China University of Technology, Guangzhou 510640, China.

出版信息

Chem Commun (Camb). 2019 Nov 12;55(91):13769-13772. doi: 10.1039/c9cc07263b.

Abstract

A palladium-catalyzed uniquely regioselective C-H alkynylation of indoles has been described. In this protocol, simple and readily available haloalkynes are employed as efficient alkynylating reagents, affording a series of functionalized 7-alkynylindoles in moderate to good yields. Moreover, further transformations of 7-alkynylated products were performed, which demonstrated the potential application of this method in organic synthesis.

摘要

本文描述了钯催化吲哚的独特区域选择性 C-H 炔基化反应。在该方案中,使用简单易得的卤代炔作为有效的炔基化试剂,以中等至良好的收率得到一系列官能化的 7-炔基吲哚。此外,还对 7-炔基化产物进行了进一步的转化,这表明该方法在有机合成中有潜在的应用。

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