Copper-Catalyzed Aerobic C(sp2)–H Functionalization for C–N Bond Formation: Synthesis of Pyrazoles and Indazoles

A simple, practical, and highly efficient synthesis of pyrazoles and indazoles via copper-catalyzed direct aerobic oxidative C(sp2)–H amination has been reported herein. This process tolerated a variety of functional groups under mild conditions. Further diversification of pyrazoles was also investi...

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Bibliographic Details
Published inJournal of organic chemistry Vol. 78; no. 8; pp. 3636 - 3646
Main Authors Li, Xianwei, He, Li, Chen, Huoji, Wu, Wanqing, Jiang, Huanfeng
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 19.04.2013
Amer Chemical Soc
Subjects
Amination
Catalysis
Chemistry
Chemistry, Organic
Copper - chemistry
Indazoles - chemical synthesis
Indazoles - chemistry
Molecular Structure
Oxidation-Reduction
Physical Sciences
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Science & Technology
OXYGEN
REARRANGEMENT
PALLADIUM
AMINATION
EFFICIENT SYNTHESIS
AMIDATION
TERMINAL ALKYNES
H BONDS
OXIDATIVE CYCLIZATION
INTERNAL ALKYNES
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Summary:A simple, practical, and highly efficient synthesis of pyrazoles and indazoles via copper-catalyzed direct aerobic oxidative C(sp2)–H amination has been reported herein. This process tolerated a variety of functional groups under mild conditions. Further diversification of pyrazoles was also investigated, which provided its potential for drug discovery.
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content type line 23
ISSN:0022-3263
1520-6904
DOI:10.1021/jo400162d