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钯催化的溴代炔烃与β-烷基苯胺的氧化C-H活化/环化反应:通往功能化3-溴吲哚的途径

Palladium-catalyzed oxidative C-H activation/annulation of -alkylanilines with bromoalkynes: access to functionalized 3-bromoindoles.

作者信息

Fang Songjia, Chen Wenhao, Jiang Huanfeng, Ma Ruize, Wu Wanqing

机构信息

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

出版信息

Chem Commun (Camb). 2022 Aug 25;58(69):9666-9669. doi: 10.1039/d2cc03298h.

DOI:10.1039/d2cc03298h
PMID:35946388
Abstract

A straightforward approach to the synthesis of 3-bromoindoles palladium-catalyzed oxidative C-H activation/annulation of -alkylanilines with bromoalkynes has been described. This protocol features high atom economy, excellent chemo- and regioselectivities, and good functional group tolerance. Moreover, the resultant 3-bromoindoles can be transformed to various functionalized indole derivatives, which demonstrates the practicability of this method in organic synthesis.

摘要

已报道了一种通过钯催化的邻烷基苯胺与溴代炔烃的氧化C-H活化/环化反应直接合成3-溴代吲哚的方法。该方法具有高原子经济性、出色的化学和区域选择性以及良好的官能团耐受性。此外,所得的3-溴代吲哚可转化为各种功能化的吲哚衍生物,这证明了该方法在有机合成中的实用性。

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