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以氯仿作为一氧化碳源,钯催化卤代取代的7-氮杂吲哚及其他杂芳烃的氨羰基化反应。

Palladium-catalyzed aminocarbonylation of halo-substituted 7-azaindoles and other heteroarenes using chloroform as a carbon monoxide source.

作者信息

Kannaboina Prakash, Raina Gaurav, Anil Kumar K, Das Parthasarathi

机构信息

Medicinal Chemistry Division, Indian Institute of Integrative Medicine (CSIR), Jammu 180001, India.

出版信息

Chem Commun (Camb). 2017 Aug 22;53(68):9446-9449. doi: 10.1039/c7cc04339b.

Abstract

A palladium-catalyzed aminocarbonylation of halo-substituted 7-azaindoles utilizing CHCl as the carbonyl source has been developed for the straightforward incorporation of an amide functional group. The protocol was extended to other heteroarenes such as pyrazolopyridines and indazoles. The substrate scope of the reaction with respect to heteroarenes and the amine component is reported. This method offers an alternative avenue for aminocarbonylation of pharmaceutically important heterocycles.

摘要

已开发出一种以CHCl作为羰基源的钯催化卤代取代7-氮杂吲哚的氨羰基化反应,用于直接引入酰胺官能团。该方法扩展到了其他杂芳烃,如吡唑并吡啶和吲唑。报道了该反应在杂芳烃和胺组分方面底物的适用范围。此方法为药学上重要的杂环的氨羰基化提供了一条替代途径。

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