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3,4-Annulated Indoles via Tandem Cyclopropane Ring-Opening/Conia-ene and Michael Addition/Conia-ene Reactions

Shane R. Cochrane, Michael A. Kerr

2022Organic Letters20 citationsDOIOpen Access PDF

Abstract

4-Alkynyl indoles, when treated with a benzylidene malonate or a donor-acceptor cyclopropane in the presence of a zinc halide, furnished 3,4-hexannylated or 3,4-heptannulated products, respectively, in fair to excellent yields. The reaction proceeds via a tandem addition/Conia-ene cyclization.

Topics & Concepts

CyclopropaneChemistryEne reactionTandemMichael reactionRing (chemistry)MalonateAcceptorHalideStereochemistryMedicinal chemistryOrganic chemistryCatalysisCondensed matter physicsComposite materialPhysicsMaterials scienceCyclopropane Reaction MechanismsCatalytic Alkyne ReactionsCatalytic C–H Functionalization Methods
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