Modular synthesis of dihydro-isoquinolines: palladium-catalyzed sequential C(sp2)-H and C(sp3)-H bond activation
Weidong Liu1,2,3, Qingzhen Yu1,2,3, Le'an Hu1,2,3
1School of Pharmaceutical Science and Technology , Tianjin University , 92 Weijin Road, Nankai District , Tianjin 300072 , China .
Abstract:
An efficient synthesis of dihydro-isoquinolines via a Pd-catalyzed double C-H bond [a C(sp2)-H and a C(sp3)-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.
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