Enantioselective α-Amination of 1,3-Dicarbonyl Compounds in Batch and Flow with Immobilized Thiourea Organocatalysts

<p> A polymer-supported bifunctional thiourea organocatalyst (<strong>PS</strong>-<strong>TU</strong>) has been prepared and successfully used in the enantioselective a-amination of 1,3-dicarbonyl compounds with azodicarboxylates. In contrast with homogeneous thioureas,...

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Detalles Bibliográficos
Autores: Kasaplar, Pinar, Ozkal, Erhan, Rodríguez-Escrich, Carles, Pericàs, Miquel A.
Tipo de recurso: artículo
Fecha de publicación:2015
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:2072/305816
Acceso en línea:http://hdl.handle.net/2072/305816
https://doi.org/10.1039/c5gc00496a
Access Level:acceso abierto
Descripción
Sumario:<p> A polymer-supported bifunctional thiourea organocatalyst (<strong>PS</strong>-<strong>TU</strong>) has been prepared and successfully used in the enantioselective a-amination of 1,3-dicarbonyl compounds with azodicarboxylates. In contrast with homogeneous thioureas, <strong>PS</strong>-<strong>TU</strong> is not irreversibly deactivated by the azodicarboxylate reagents, and simple washing with triethylamine between runs has allowed the repeated reuse (9 cycles) of the <strong>PS</strong>-<strong>TU</strong> catalyst. The a-amination mediated by <strong>PS</strong>-<strong>TU</strong> has also been adapted to perform the enantioselective amination (93% ee) of ethyl 2-oxocyclopentanecarboxylate in continuous flow (7.5 h operation, 21 min residence time, TON = 37).</p>