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铑催化的室温下喹啉 N-氧化物与三氟乙酰胺的 C8-H 区域选择性胺化反应。

Rhodium-catalyzed regioselective C8-H amination of quinoline N-oxides with trifluoroacetamide at room temperature.

机构信息

College of Chemistry and Molecular Engineering, Zhengzhou University, 75 Daxue Street, Zhengzhou, Henan Province 450052, China.

出版信息

Org Biomol Chem. 2018 Jul 7;16(25):4728-4733. doi: 10.1039/c8ob01108g. Epub 2018 Jun 14.

Abstract

A facile and efficient protocol for rhodium-catalyzed amination of quinoline N-oxides at the C-8 position using simple and commercially available trifluoroacetamide as the amino source has been developed, which proceeds with perfect regioselectivity at room temperature and short reaction times. This catalytic system is highly convenient on a gram scale. The desired products feature diverse functional group tolerance with good to excellent yields.

摘要

开发了一种简便高效的铑催化喹啉 N-氧化物 C-8 位胺化反应的方法,使用简单易得的三氟乙酰胺作为氨基源。该反应在室温下,具有完美的区域选择性,反应时间短。该催化体系在克级规模下非常方便。目标产物具有广泛的官能团容忍性,产率良好至优秀。

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