当前位置: X-MOL 学术Angew. Chem. Int. Ed. › 论文详情
Cobalt-Catalyzed Electrophilic Amination of Aryl- and Heteroarylzinc Pivalates with N-Hydroxylamine Benzoates
Angewandte Chemie International Edition ( IF 12.102 ) Pub Date : 2017-12-28 , DOI: 10.1002/anie.201710931
Yi-Hung Chen, Simon Graßl, Paul Knochel

Abstract

Aryl- and heteroarylzinc pivalates can be aminated with O-benzoylhydroxylamines at 25 °C within 2–4 h in the presence of 2.5–5.0 % CoCl2⋅2 LiCl to furnish the corresponding tertiary arylated or heteroarylated amines in good yields. This electrophilic amination also provides access to diarylamines and aryl(heteroaryl)amines. A new tuberculosis drug candidate (Q203) was prepared in six steps and 56 % overall yield by using this cobalt-catalyzed amination as the key step.

Thumbnail image of graphical abstract

Animating aminations: A range of aryl- and heteroarylzinc pivalates underwent cobalt-catalyzed electrophilic aminations with O-benzoylhydroxylamines in good yields under mild conditions. This reaction can be applied to prepare arylamines and diarylamines. A new tuberculosis drug candidate was prepared in six steps and 56 % overall yield by using the cobalt-catalyzed amination as the key step.

更新日期:2018-01-16

 

分享到
评论: 1
期刊列表
华中师范大学化学生物学研究中心诚聘质谱实验员
西湖大学邓力教授课题组招聘启事
天合科研
【问答】请问制备有机锌试剂需要注意哪些问题?
2017年中科院JCR分区化学大类列表
试剂库存管理
化合物查询
down
wechat
bug