Pd-catalysed amidation of 2,6-dihalopurine nucleosides. Replacement of iodine at 0 ºC

Pd-catalysed reactions of 2-Cl, 2-Br and 2-I derivatives of a 6-chloropurine nucleoside with benzamide have been compared, using Pd2dba3, Xantphos and Cs2CO3 in toluene, between 20 and 80 °C. The reactivity order was 2-I > 2-Br > 6-Cl ≫ 2-Cl. The 2-I substituent could be replaced even at 0 °C,...

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Detalles Bibliográficos
Autores: Bosch Hereu, Lluís, Cialîcu, Ionela, Caner, Joaquim, Ariza Piquer, Xavier, Costa i Arnau, Anna M., Terrazas Martínez, Montserrat, Vilarrasa i Llorens, Jaume
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2012
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:2445/53208
Acceso en línea:https://hdl.handle.net/2445/53208
Access Level:acceso abierto
Palabra clave:Àcids nucleics
Compostos heterocíclics
Citotoxicitat per mediació cel·lular
Nucleòsids
Medicaments antineoplàstics
Nucleic acids
Heterocyclic compounds
Cell-mediated cytotoxicity
Nucleosides
Antineoplastic agents
Descripción
Sumario:Pd-catalysed reactions of 2-Cl, 2-Br and 2-I derivatives of a 6-chloropurine nucleoside with benzamide have been compared, using Pd2dba3, Xantphos and Cs2CO3 in toluene, between 20 and 80 °C. The reactivity order was 2-I > 2-Br > 6-Cl ≫ 2-Cl. The 2-I substituent could be replaced even at 0 °C, under conditions disclosed here for the first time. On the other hand, the replacement of the chlorine atom at position 2 (2-Cl) required 110 °C.