期刊
SCIENCE CHINA-CHEMISTRY
卷 -, 期 -, 页码 -出版社
SCIENCE PRESS
DOI: 10.1007/s11426-023-1785-1
关键词
Rh-catalysis; azaindoles; pyridyl Csp(2)-H bond; carboamination; coupling-cyclization
The development of a Rh-catalyzed amine-directed remote 5,6-carboamination protocol of pyridines via dual Csp(2)-H functionalizations is disclosed in this study. Various readily available 2-aminopyridines and 1,2,3-triazoles can be coupled and cyclized to access polyfunctionalized azaindoles. Mechanistic studies reveal the involvement of relay carbenoid-electrophilic addition to pyridines and sequential pyridyl Csp(2)-H amination in this transformation. The post-synthetic utility of this methodology is demonstrated through versatile and site-selective modification of azaindoles.
We disclose the development of the Rh-catalyzed amine-directed remote 5,6-carboamination protocol of pyridines via dual Csp(2)-H functionalizations. A variety of readily available 2-aminopyridines and 1,2,3-triazoles are allowed for coupling cyclization to access polyfunctionalized azaindoles. Mechanistic studies including DFT calculations unveil that relay carbenoid-electrophilic addition to pyridines and the sequential pyridyl Csp(2)-H amination are involved in this transformation. The post-synthetic utility of this methodology is showcased by versatile and site-selective modification of azaindoles.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据