Modular synthesis of dihydro-isoquinolines: palladium-catalyzed sequential C(sp2)-H and C(sp3)-H bond activation

被引:29
作者
Liu, Weidong [1 ,2 ,3 ]
Yu, Qingzhen [1 ,2 ,3 ]
Hu, Le'an [1 ,2 ,3 ]
Chen, Zenghua [1 ,2 ,3 ]
Huang, Jianhui [1 ,2 ,3 ]
机构
[1] Tianjin Univ, Sch Pharmaceut Sci & Technol, Tianjin 300072, Peoples R China
[2] Collaborat Innovat Ctr Chem Sci & Engn Tianjin, Tianjin 300072, Peoples R China
[3] Tianjin Key Lab Modern Drug Delivery & High Effic, Tianjin, Peoples R China
基金
中国国家自然科学基金;
关键词
C-H ACTIVATION; ORGANOMETALLIC CHEMISTRY; FUNCTIONALIZATION; DERIVATIVES; ARYLATION; ALKYL;
D O I
10.1039/c5sc01482d
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An efficient synthesis of dihydro-isoquinolines via a Pd-catalyzed double C-H bond [a C(sp(2))-H and a C(sp(3))-H bond] activation/annulation (CHAA) reaction is presented. This methodology features a short reaction time, high atom economy (loss of H2O only) and the formation of a sterically less favoured tertiary C-N bond. This fast (30 min) and environmentally benign radical C-H activation approach has demonstrated the potential direction for the future design/development of fast and efficient C-H direct functionalization processes.
引用
收藏
页码:5768 / 5772
页数:5
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