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Palladium‐Catalyzed Cascade Carbonylation to α,β‐Unsaturated Piperidones via Selective Cleavage of Carbon–Carbon Triple Bonds

Yao Ge, Fei Ye, Ji Yang, Anke Spannenberg, Haijun Jiao, Ralf Jackstell, Matthias Beller

2021Angewandte Chemie International Edition25 citationsDOIOpen Access PDF

Abstract

A direct and selective synthesis of α,β-unsaturated piperidones by a new palladium-catalyzed cascade carbonylation is described. In the presented protocol, easily available propargylic alcohols react with aliphatic amines to provide a broad variety of interesting heterocycles. Key to the success of this transformation is a remarkable catalytic cleavage of the present carbon-carbon triple bond by using a specific catalyst with 2-diphenylphosphinopyridine as ligand and appropriate reaction conditions. Mechanistic studies and control experiments revealed branched unsaturated acid 11 as crucial intermediate.

Topics & Concepts

CarbonylationPalladiumCatalysisReinforced carbon–carbonCascadeChemistryTriple bondCarbon fibersCleavage (geology)Organic chemistryCombinatorial chemistryCarbon monoxideMaterials scienceDouble bondComposite numberChromatographyFracture (geology)Composite materialCatalytic C–H Functionalization MethodsCyclopropane Reaction MechanismsSynthetic Organic Chemistry Methods
Palladium‐Catalyzed Cascade Carbonylation to α,β‐Unsaturated Piperidones via Selective Cleavage of Carbon–Carbon Triple Bonds | Litcius