Preparation of substituted tetrahydroisoquinolines by Pd(II)-catalyzed NH2-directed insertion of Michael acceptors into C-H bonds followed by NH2-conjugated additions

3,3-Disubstituted tetrahydroisoquinolines are prepared in one step from Michael acceptors and 2-phenylethylamines under Pd catalysis and Ag2CO3 as an oxidant. Presumably, activation of an ortho C-H bond of the aromatic ring with Pd(II) is directed by the primary amine to form a palladacycle. Inserti...

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Detalles Bibliográficos
Autores: Mancinelli, Andrea, Alamillo, Carla, Albert Mach, Joan, Ariza Piquer, Xavier, Etxabe, Haizea, Farràs i Soler, Jaume, García Gómez, Jordi, Granell Sanvicente, Jaime Ramón, Quijada, F. Javier
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2017
País:España
Institución:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/107929
Acceso en línea:https://hdl.handle.net/2445/107929
Access Level:acceso abierto
Palabra clave:Compostos heterocíclics
Pal·ladi (Element químic)
Catàlisi
Heterocyclic compounds
Palladium
Catalysis
Descripción
Sumario:3,3-Disubstituted tetrahydroisoquinolines are prepared in one step from Michael acceptors and 2-phenylethylamines under Pd catalysis and Ag2CO3 as an oxidant. Presumably, activation of an ortho C-H bond of the aromatic ring with Pd(II) is directed by the primary amine to form a palladacycle. Insertion of the olefin, subsequent conjugated addition of the amine, and reductive elimination of Pd(0) affords the expected products. Silver carbonate is not necessary when 2-phenylethylamines are converted previously to N-benzoyloxy-2-phenylethylamines.