Diastereo- and Enantioselective Organocatalytic Synthesis of Spirocyclopropyl Pyrazolones

[EN] A diastereo- and enantioselective synthesis of spirocyclopropylpyrazolones has been described through a Michael/alkylation cascade reaction of 4-arylidenepyrazol-5-ones with diethyl 2-bromomalonate catalyzed by (DHQ)(2)AQN. The reaction afforded selectively the corresponding spirocyclic compoun...

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Detalles Bibliográficos
Autores: Carceller-Ferrer, Laura, Blay, Gonzalo, Pedro, José R., Vila, Carlos, Muñoz Roca, María Del Carmen|||0000-0003-2630-3897
Tipo de recurso: artículo
Fecha de publicación:2024
País:España
Institución:Universitat Politècnica de València (UPV)
Repositorio:RiuNet. Repositorio Institucional de la Universitat Politécnica de Valéncia
Idioma:inglés
OAI Identifier:oai:riunet.upv.es:10251/220278
Acceso en línea:https://riunet.upv.es/handle/10251/220278
Access Level:acceso abierto
Palabra clave:Spirocyclic compounds
Pyrazolones
Cyclopropanes
Organocatalysis
Asymmetric synthesis
Descripción
Sumario:[EN] A diastereo- and enantioselective synthesis of spirocyclopropylpyrazolones has been described through a Michael/alkylation cascade reaction of 4-arylidenepyrazol-5-ones with diethyl 2-bromomalonate catalyzed by (DHQ)(2)AQN. The reaction afforded selectively the corresponding spirocyclic compounds with 30-83% yield, diastereoselectivities ranging from 60:40 to >95:5 and 26-93% enantiomeric excess under mild reaction conditions. Moreover, we performed two selective transformations with the corresponding chiral compounds.