Ruthenium(II)-Catalyzed C-H Bond Regioselective [3+2] Annulation of Arylamines with Propargyl Alcohols

被引:2
|
作者
Bai, Lili [1 ]
Wang, Ying [1 ]
Wang, Shuojin [1 ]
Kong, Dulin [1 ]
Fu, Yan [1 ]
Peng, Deqian [1 ]
Wen, Lijun [1 ]
Chen, Xun [1 ]
机构
[1] Hainan Med Univ, Sch Pharm, Haikou 571199, Hainan, Peoples R China
关键词
ruthenium(II); C-H bond; regioselective; annulation reaction; N-BOND; INDOLE SYNTHESIS; FUNCTIONALIZATION; CYCLIZATION;
D O I
10.6023/cjoc201806039
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A simple and efficient ruthenium(II)-catalyzed C-H bond regioselective [3+2] annulation of arylamines with propargyl alcohols has been reported. This protocol provides a facile approach to hydroxy-containing indole skeleton, which could be employed for constructing more complex and useful pharmaceutical molecules. Meantime, the kinetic isotope effect was further investigated and the results indicated that the C-H bond-breaking was possibly involved in the rate-limiting step of this transformation.
引用
收藏
页码:3242 / 3249
页数:8
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