钯催化1-萘胺与酰氯的C8-H酰化反应
Palladium-Catalyzed C8-H Acylation of 1-Naphthylamines with Acyl Chlorides.
作者信息
Yu Xiaomeng, Yang Fan, Wu Yusheng, Wu Yangjie
机构信息
The College of Chemistry and Molecular Engineering, Henan Key Laboratory of Chemical Biology and Organic Chemistry, Key Laboratory of Applied Chemistry of Henan Universities , Zhengzhou University , Zhengzhou 450052 , People's Republic of China.
Tetranov Biopharm , LLC & Collaborative Innovation Center of New Drug Research and Safety Evaluation , Zhengzhou 450052 , People's Republic of China.
出版信息
Org Lett. 2019 Mar 15;21(6):1726-1729. doi: 10.1021/acs.orglett.9b00283. Epub 2019 Mar 7.
A facile and efficient protocol for palladium-catalyzed regioselective C8-H acylation of 1-naphthylamine derivatives with acyl chlorides has been developed. The reaction exhibits broad functional group tolerance, and both aromatic and α,β-unsaturated acyl chlorides can be effectively coupled with 1-naphthylamines. Moreover, the picolinamide moiety as a bidentate directing likely plays a key role in this regioselective transformation.
已开发出一种简便高效的钯催化1-萘胺衍生物与酰氯进行区域选择性C8-H酰化反应的方法。该反应对官能团具有广泛的耐受性，芳香族和α,β-不饱和酰氯均可与1-萘胺有效偶联。此外，作为双齿导向基团的吡啶甲酰胺部分可能在这种区域选择性转化中起关键作用。
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