Synthesis of aza-fused polycyclic quinolines via double C-H bond activation |
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| Authors: | Huang Ji-Rong Dong Lin Han Bo Peng Cheng Chen Ying-Chun |
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| Affiliation: | Key Laboratory of Drug-Targeting and Drug Delivery Systems of the Ministry of Education, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, 17/3 South Renmin Road, Chengdu, 610041, PR China. |
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| Abstract: | Simple but efficient: Aza-fused polycyclic quinolines were efficiently assembled through rhodium(III)-based direct double C-H activation of N-aryl azoles followed by cyclization with alkynes without heteroatom-assisted chelation. Copper(II) acetate, aside from acting as an oxidant, could also play an important role in the C-H activation process. |
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