Enantioselective synthesis of indole derivatives by Rh/Pd relay catalysis and their anti-inflammatory evaluation.
- Resource Type
- Article
- Authors
- Li, Sifeng; Wang, Zihao; Xiao, Haitao; Bian, Zhaoxiang; Wang, Jun (Joelle)
- Source
- Chemical Communications. 7/14/2020, Vol. 56 Issue 55, p7573-7576. 4p.
- Subject
- *INDOLE derivatives
*CATALYSIS
*HYDROAMINATION
*LEAD compounds
*INDOLE
- Language
- ISSN
- 1359-7345
An efficient Rh/Pd relay catalyzed intermolecular and cascade intramolecular hydroamination for the synthesis of exclusive trans 1-indolyl dihydronaphthalenols (up to 88% yield, 99% ee) is described under mild conditions. Moreover, the in silico and in vitro screening showed that the novel 1-indolyl dihydronaphthalenol products are potent lead compounds for treating inflammation disease. [ABSTRACT FROM AUTHOR]