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

Sifeng Li, Zihao Wang, Haitao Xiao, Zhaoxiang Bian, Jun Wang

2020Chemical Communications34 citationsDOI

Abstract

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.

Topics & Concepts

Enantioselective synthesisIndole testCatalysisCombinatorial chemistryChemistrySynergistic catalysisRelayOrganic chemistryPower (physics)Quantum mechanicsPhysicsCatalytic C–H Functionalization MethodsSynthesis of Indole DerivativesAxial and Atropisomeric Chirality Synthesis
Enantioselective synthesis of indole derivatives by Rh/Pd relay catalysis and their anti-inflammatory evaluation | Litcius