Enantioselective synthesis of indole derivatives by Rh/Pd relay catalysis and their anti-inflammatory evaluation

被引:28
|
作者
Li, Sifeng [1 ,2 ]
Wang, Zihao [1 ,2 ]
Xiao, Haitao [3 ]
Bian, Zhaoxiang [2 ]
Wang, Jun [1 ]
机构
[1] Southern Univ Sci & Technol, Dept Chem, Shenzhen 518055, Peoples R China
[2] Hong Kong Baptist Univ, Sch Chinese Med, Hong Kong, Peoples R China
[3] Shenzhen Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Shenzhen 518066, Peoples R China
关键词
RING-OPENING REACTION; ONE-POT SYNTHESIS; BIOLOGICAL EVALUATION; ASYMMETRIC-SYNTHESIS; IN-VITRO; OXABENZONORBORNADIENES; PALLADIUM; METAL; DESIGN; CYCLIZATION;
D O I
10.1039/d0cc03158e
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An efficient Rh/Pd relay catalyzed intermolecular and cascade intramolecular hydroamination for the synthesis of exclusivetrans1-indolyl dihydronaphthalenols (up to 88% yield, 99% ee) is described under mild conditions. Moreover, thein silicoandin vitroscreening showed that the novel 1-indolyl dihydronaphthalenol products are potent lead compounds for treating inflammation disease.
引用
收藏
页码:7573 / 7576
页数:4
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