Copper(II)‐Catalyzed Selective Para Amination of Arylamine with Pyrazole by C−H Functionalization

A coordinating activation strategy for selective para amination of arylamine with pyrazole is developed. Various substrates are compatible, giving the corresponding products in moderate to good yields. This strategy provides a practical solution for the efficient synthesis of arylamine‐containing ph...

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Bibliographic Details
Published in:ChemCatChem 2018-09, Vol.10 (17), p.3675-3679
Main Authors: Xu, Jun, Du, Kui, Shen, Jiabin, Shen, Chao, Chai, Kejie, Zhang, Pengfei
Format: Article
Language:English
Subjects:
Aniline
Copper
Copper compounds
C−H Functionalization
Electron transfer
Naphthylamine
Pharmacology
Pyrazole
Substrates
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Summary:A coordinating activation strategy for selective para amination of arylamine with pyrazole is developed. Various substrates are compatible, giving the corresponding products in moderate to good yields. This strategy provides a practical solution for the efficient synthesis of arylamine‐containing pharmacophores from simple starting materials. A single electron transfer mechanism is suggested for this reaction. Sourcing nitrogen: N‐containing compounds are highly valuable skeletons with many applications. It is of great importance to develop general and efficient methodologies for the construction of C−N bond. Here, a coordinating activation strategy for selective para amination of arylamine with pyrazole is developed, providing a practical solution for the efficient synthesis of arylamine‐containing pharmacophores from simple starting materials.
ISSN:1867-3880
1867-3899
DOI:10.1002/cctc.201800328