二氢异喹啉的模块化合成：钯催化的连续C(sp)-H和C(sp)-H键活化

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

作者信息

Liu Weidong, Yu Qingzhen, Hu Le'an, Chen Zenghua, Huang Jianhui

机构信息

School of Pharmaceutical Science and Technology , Tianjin University , 92 Weijin Road, Nankai District , Tianjin 300072 , China . Email:

Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Tianjin 300072 , China.

出版信息

Chem Sci. 2015 Oct 1;6(10):5768-5772. doi: 10.1039/c5sc01482d. Epub 2015 Jun 26.

An efficient synthesis of dihydro-isoquinolines a Pd-catalyzed double C-H bond [a C(sp)-H and a C(sp)-H bond] activation/annulation (CHAA) reaction is presented. This methodology features a short reaction time, high atom economy (loss of HO 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.