期刊
ORGANIC LETTERS
卷 24, 期 20, 页码 3614-3619出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.2c01140
关键词
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资金
- National Natural Science Foundation of China [22178078, 21871071]
- Ten-Thousand Talents Plan of Zhejiang Province [2019R51012]
This study presents a simple and mild method for the chemoselective mono- and diamination of ketones using pyrazole as the amine source in a combined copper-organocatalyst system. The strategy offers an efficient and convenient solution for synthesizing alpha-pyrazole and alpha,alpha-dipyrazole ketone derivatives, with moderate to good yields. The control experiment confirms the key intermediate of in situ generated hydrazone in the transformation.
Herein, we report a simple and mild protocol for the chemoselective mono- and diamination of ketone using pyrazole as the amine source in a combined copper-organocatalyst system. Various substrates are compatible, providing the corresponding products in moderate to good yields. This strategy gives an efficient and convenient solution for the synthesis of alpha-pyrazole and alpha,alpha-dipyrazole ketone derivatives. The control experiment demonstrates that in situ generated hydrazone is a key intermediate in the transformation.
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