CuBr-catalyzed direct indolation of tetrahydroisoquinolines via cross-dehydrogenative coupling between sp3 C-H and sp2 C-H bonds.

作者: Zhiping Li , Chao-Jun Li

DOI: 10.1021/JA0516054

关键词: ReagentMedicinal chemistryCopper bromideCatalysisCoupling (electronics)Bicyclic moleculeChemistryDehydrogenationStereochemistryOxidizing agentReaction mechanism

摘要: A novel and efficient C-C bond formation method was developed via the cross-dehydrogenative coupling (CDC) reaction of indoles tetrahydroisoquinolines catalyzed by copper bromide in presence an oxidizing reagent, tert-BuOOH. The CDC provides a simple catalytic to construct indolyl combination sp3 C-H sp2 followed formation.

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