Room-Temperature CuI-Catalyzed N-Arylation of Cyclopropylamine

Peng Hong,Xinhai Zhu, Xin Lai, Zinan Gong,Manna Huang,Yiqian Wan

JOURNAL OF ORGANIC CHEMISTRY(2023)

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摘要
A general and efficient CuI/N-carbazolyl-1H-pyrrole-2-carbohydrazide catalyst system was developed for the N-arylation of cyclopropylamine using aryl bromides at room temperature. Herein, 5 mol % CuI and 5 mol % of the ligand were used to synthesize N-aryl cyclopropylamines in moderate to excellent yields. This protocol was scaled up to produce the desired product at gram levels and has been generalized for C-N coupling between aryl bromides and amines at room temperature.
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