Hong Peng, Zhu Xinhai, Lai Xin, Gong Zinan, Huang Manna, Wan Yiqian
School of Chemical Engineering and Technology, Sun Yat-sen University, Zhuhai 519082, P. R. China.
Guangdong Engineering Technology Research Center for Platform Chemicals from Marine Biomass and Their Functionalization, Sun Yat-sen University, Zhuhai 519082, P. R. China.
J Org Chem. 2024 Jan 5;89(1):57-67. doi: 10.1021/acs.joc.3c01357. Epub 2023 Dec 18.
A general and efficient CuI/-carbazolyl-1-pyrrole-2-carbohydrazide catalyst system was developed for the -arylation of cyclopropylamine using aryl bromides at room temperature. Herein, 5 mol % CuI and 5 mol % of the ligand were used to synthesize -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.
开发了一种通用且高效的碘化亚铜/咔唑基-1-吡咯-2-碳酰肼催化剂体系，用于在室温下使用芳基溴化物对环丙胺进行芳基化反应。在此，使用5摩尔%的碘化亚铜和5摩尔%的配体以中等至优异的产率合成芳基环丙胺。该方案放大至克级规模制备所需产物，并且已推广用于室温下芳基溴化物与胺之间的碳氮偶联反应。
