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[4 + 2] Cyclization or Lossen Rearrangement: Rhodium-Catalyzed Divergent Synthesis of Carboline Derivatives with Anticancer Activity

Lijie Lv, Jia Zheng, Yijie Xiao, Dan Ni, Zhangshun Luo, Yunyun Gao, Yue Wei, Yi He, Shenyou Nie

2024Organic Letters21 citationsDOI

Abstract

An unusual rhodium-catalyzed C-H activation/Lossen rearrangement/oxa-Michael addition tandem cyclization has been achieved along with a tunable well-known C-H activation/[4 + 2] annulation, leading to regio-, chemo-, and diastereoselective access to diverse pentacyclic α-carbolines and β-carboline-1-one derivatives in moderate to good yields with significant anticancer activity.

Topics & Concepts

ChemistryRhodiumCatalysisCombinatorial chemistryStereochemistryMedicinal chemistryOrganic chemistryCatalytic C–H Functionalization MethodsSynthesis and bioactivity of alkaloidsCatalytic Cross-Coupling Reactions
[4 + 2] Cyclization or Lossen Rearrangement: Rhodium-Catalyzed Divergent Synthesis of Carboline Derivatives with Anticancer Activity | Litcius