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芳基重氮盐和重氮酯原位生成腈亚胺:室温下全取代吡唑的合成。

In Situ Generation of Nitrilimines from Aryldiazonium Salts and Diazo Esters: Synthesis of Fully Substituted Pyrazoles under Room Temperature.

机构信息

Jiangsu Key Laboratory of Advanced Catalytic Materials and Technology, Advanced Catalysis and Green Manufacturing Collaborative Innovation Center , Changzhou University , Changzhou 213164 , P. R. China.

Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science , Soochow University , Suzhou 215123 , P. R. China.

出版信息

Org Lett. 2018 Apr 20;20(8):2412-2415. doi: 10.1021/acs.orglett.8b00750. Epub 2018 Apr 6.

Abstract

A novel one-pot synthesis for fully substituted pyrazoles has been well developed via the in situ generation of nitrilimines from aryldiazonium salts and diazo esters and a subsequent cycloaddition with 1,3-dicarbonyl compounds. High yields, mild conditions, wide substrate scope, and operational simplicity are the significant advantages of this methodology.

摘要

通过芳基重氮盐与重氮酯原位生成亚胺氮宾,然后与 1,3-二羰基化合物进行后续环加成反应,开发了一种新型一锅法合成完全取代的吡唑的方法。该方法具有产率高、条件温和、底物范围广、操作简单等显著优点。

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