An Xiao-De, Duan Kang, Li Xian-Jiang, Yang Jian-Ming, Lu Yong-Na, Liu Qing, Xiao Jian
Shandong Kangqiao Biotechnology Co. Ltd. , Binzhou 256500 , China.
School of Chemistry and Molecular Engineering , Nanjing Tech University , Nanjing 211816 , China.
J Org Chem. 2019 Sep 20;84(18):11839-11847. doi: 10.1021/acs.joc.9b01703. Epub 2019 Sep 5.
A Brønsted acid-catalyzed α-C(sp)-H amination of cyclic amines using hydrazines as coupling partners has been reported. This methodology provides a unique protocol to the one-step assembly of tetrahydro[1,3,4]triazepines via [1,5]-hydride transfer-initiated C(sp)-H amination. This reaction features mild conditions, good yields, and high atom economy.
据报道，使用肼作为偶联伙伴，通过布朗斯特酸催化的环状胺的α-C(sp)-H胺化反应。该方法为通过[1,5]-氢转移引发的C(sp)-H胺化一步组装四氢[1,3,4]三氮杂卓提供了一种独特的方案。该反应具有条件温和、产率高和原子经济性高的特点。
