Room-Temperature CuI-Catalyzed N-Arylation of Cyclopropylamine,The Journal of Organic Chemistry

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Room-Temperature CuI-Catalyzed N-Arylation of Cyclopropylamine
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2023-12-18 , DOI: 10.1021/acs.joc.3c01357
Peng Hong _{1,

2} , Xinhai Zhu _{2,

3} , Xin Lai _{1,

2} , Zinan Gong ₁ , Manna Huang _{1,

2} , Yiqian Wan _{1,

2}

Affiliation

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.

中文翻译：

室温 CuI 催化环丙胺的 N-芳基化

开发了一种通用且高效的 CuI/ N-咔唑基-1H-吡咯-2-碳酰肼催化剂体系，用于在室温下使用芳基溴进行环丙胺的N-芳基化。在此，使用 5 mol% CuI 和 5 mol% 配体以中等至优异的产率合成N-芳基环丙胺。该方案被放大以生产克级的所需产物，并已推广到室温下芳基溴和胺之间的 C-N 偶联。

更新日期：2023-12-18

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