Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 19, Issue 39, Pages 8497-8501Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1ob01561c
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Funding
- Science & Engineering Research Board (SERB), Department of Science and Technology (DST), India [EMR/2017/002601]
- CSIR
- CSIR-IICT [IICT/Pubs./2021/248]
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This study presents a novel copper-catalyzed tandem reaction for the efficient synthesis of a specific three-ring compound, which has been successfully applied to the total synthesis of the anticancer drug TIC10/ONC201.
Herein, we present a copper-catalyzed tandem reaction of 2-aminoimidazolines and ortho-halo(hetero)aryl carboxylic acids that causes the regioselective formation of angularly fused tricyclic 1,2-dihydroimidazo[1,2-a]quinazolin-5(4H)-one derivatives. The reaction involved in the construction of the core six-membered pyrimidone moiety proceeded via regioselective N-arylation-condensation. The presented protocol been successfully applied to accomplish the total synthesis of TIC10/ONC201, which is an active angular isomer acting as a tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL): a sought after anticancer clinical agent.
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