Palladium-catalyzed intramolecular C–H arylation of 2-halo-N-Boc-N-arylbenzamides for the synthesis of N–H phenanthridinones |
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| Authors: | Quan-Fang Hu Tian-Tao Gao Yao-Jie Shi Qian Lei Luo-Ting Yu |
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| Affiliation: | State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University and Collaborative Innovation Center, Chengdu 610041 China, Fax: +86-28-85164060, +86-28-85164063 |
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| Abstract: | A palladium catalyzed synthesis of N–H phenanthridinones was developed via C–H arylation. The protocol gives phenanthridinones regioselectively by one-pot reaction without deprotection. It exhibits broad substrate scope and affords targets in up to 95% yields. Importantly, it could be applied for the less reactive o-chlorobenzamides.Pd(t-Bu3P)2/KOAc proved to be a good combination for one-pot synthesis of N–H phenanthridinones with up to 95% yield. |
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