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


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.

SUBMITTER: Liu W 

PROVIDER: S-EPMC5950195 | biostudies-other | 2015 Oct

REPOSITORIES: biostudies-other

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Modular synthesis of dihydro-isoquinolines: palladium-catalyzed sequential C(sp<sup>2</sup>)-H and C(sp<sup>3</sup>)-H bond activation.

Liu Weidong W   Yu Qingzhen Q   Hu Le'an L   Chen Zenghua Z   Huang Jianhui J  

Chemical science 20150626 10


An efficient synthesis of dihydro-isoquinolines <i>via</i> a Pd-catalyzed double C-H bond [a C(sp<sup>2</sup>)-H and a C(sp<sup>3</sup>)-H bond] activation/annulation (CHAA) reaction is presented. This methodology features a short reaction time, high atom economy (loss of H<sub>2</sub>O 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 desig  ...[more]

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