双环[1.1.0]丁烷与烯酰胺的环加成反应用于高效合成2-氨基双环[2.1.1]己烷。
Cycloaddition of bicyclo[1.1.0]butanes with enamides for the efficient synthesis of 2-amino-bicyclo[2.1.1]hexanes.
作者信息
Zhu Yanren, Yang Shaoxiong, Chen Huiyu, Zhang Fang, Pu Enfan, Jiang Piaopiao, Jin Yi, Zhang Hongbin, Chen Jingbo
机构信息
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, Yunnan Key Laboratory of Research and Development for Natural Products, School of Pharmacy, Yunnan University, Kunming, 650500, P. R. China.
Department of Chemical Engineering, KU Leuven, Celestijnenlaan 200F, Leuven 3001, Belgium.
出版信息
Chem Commun (Camb). 2025 Jul 24;61(61):11493-11496. doi: 10.1039/d5cc02908b.
Here, we develop a mild and scalable approach for the synthesis of 2-amino-bicyclo[2.1.1]hexanes Lewis acid-catalyzed (3+2) cycloaddition of bicyclo[1.1.0]butanes (BCBs) with enamides. The practicality of this methodology has been demonstrated by scale-up reactions and product modifications, providing highly valuable aniline bioisosteres and structurally complex three-dimensional cyclic amines.
在此，我们开发了一种温和且可扩展的方法来合成2-氨基双环[2.1.1]己烷，即通过双环[1.1.0]丁烷（BCB）与烯酰胺的路易斯酸催化（3+2）环加成反应。这种方法的实用性已通过放大反应和产物修饰得到证明，可提供高价值的苯胺生物电子等排体和结构复杂的三维环状胺。
Zotero 插件