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

来源：

CHEMICAL SCIENCE | 2015年 / 6卷 / 10期

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

页码：5768 / 5772

页数：5