Concise and very efficient synthesis of the N-methylwelwistatin tetracyclic core based on an anionic domino process

An efficient synthesis of the N-methylwelwistatin tetracyclic core in only two steps from Kornfeld's ketone is described, whose key transformation involves the generation of a fused bicyclo[4.3.1]decane ring system through a one-pot sequence comprising a Michael-intramolecular aldolization anio...

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Detalles Bibliográficos
Autores: Ruiz Serrano, Miriam, López-Alvarado Gutiérrez, María Pilar, Menéndez Ramos, José Carlos
Tipo de recurso: artículo
Fecha de publicación:2010
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/128965
Acceso en línea:https://hdl.handle.net/20.500.14352/128965
Access Level:acceso abierto
Palabra clave:615:54
615.31
661.185
N-methylwelwistatin
Domino process
Synthesis
Química farmaceútica
Química orgánica (Farmacia)
2306.90 Química de Productos Naturales Orgánicos
2306 Química Orgánica
Descripción
Sumario:An efficient synthesis of the N-methylwelwistatin tetracyclic core in only two steps from Kornfeld's ketone is described, whose key transformation involves the generation of a fused bicyclo[4.3.1]decane ring system through a one-pot sequence comprising a Michael-intramolecular aldolization anionic domino process and a DBU-promoted hydrolysis of the N-pivaloyl protecting group. Besides providing the most efficient synthesis of the welwistatin core to date, this method has the advantage of installing an oxygenated function at the welwistatin D ring.