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

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

DOI: 10.1039/C5SC01482D

关键词: PalladiumMedicinal chemistryHydrogen bondSteric effectsAnnulationAtom economyPhotochemistryCatalysisChemistry

摘要: An efficient synthesis of dihydro-isoquinolines via a Pd–catalyzed double C–H bond [a C(sp2)–H and C(sp3)–H bond] activation/annulation (CHAA) reaction is presented. This methodology features short time, high atom economy (loss H2O only) the formation sterically less favoured tertiary C–N bond. fast (30 min) environmentally benign radical activation approach has demonstrated potential direction for future design/development direct functionalization processes.

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