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以杂环烯酮缩胺为配体的铜催化串联反应合成吡唑并[5,1-a]异喹啉类化合物

Copper-Catalyzed Tandem Reactions for Synthesis of Pyrazolo[5,1-a]isoquinolines with Heterocyclic Ketene Aminals as Ligands.

作者信息

Wen Li-Rong, Jin Xian-Jun, Niu Xiao-Dong, Li Ming

机构信息

State Key Laboratory Base of Eco-Chemical Engineering, College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology, Qingdao 266042, People's Republic of China.

出版信息

J Org Chem. 2015 Jan 2;80(1):90-8. doi: 10.1021/jo5020323. Epub 2014 Dec 10.

Abstract

A CuI-catalyzed tandem reaction of 5-(2-bromoaryl)-N-aryl-1H-pyrazol-3-amines with active acetonitrile derivatives to prepare pyrazolo[5,1-a]isoquinolines in good to excellent yields has been successfully developed under mild conditions with heterocyclic ketene aminals (HKAs) as new ligands. This is the first time HKAs have been used as ligands for copper-catalyzed coupling reactions.

摘要

在温和条件下,以杂环烯酮缩胺(HKAs)作为新配体,成功开发了一种CuI催化的5-(2-溴芳基)-N-芳基-1H-吡唑-3-胺与活性乙腈衍生物的串联反应,用于制备吡唑并[5,1-a]异喹啉,产率良好至优异。这是首次将HKAs用作铜催化偶联反应的配体。

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