A general methodology for the enantioselective synthesis of 1-substituted tetrahydroisoquinoline alkaloids

Starting from tricyclic lactam 2 , which is easily accessible by cyclocondensation of δ‐oxoester 1 with (R )‐phenylglycinol, a three‐step synthetic route to enantiopure 1‐substituted tetrahydroisoquinolines, including 1‐alkyl‐, 1‐aryl‐, and 1‐benzyltetrahydroisoquinoline alkaloids, as well as the tr...

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Detalhes bibliográficos
Autores: Amat Tusón, Mercedes, Elias, Viviane, Llor Brunés, Núria, Subrizi, Fabiana, Molins i Grau, Elies, Bosch Cartes, Joan
Formato: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2010
País:España
Recursos: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:2445/164357
Acesso em linha:https://hdl.handle.net/2445/164357
Access Level:acceso abierto
Palavra-chave:Alcaloides
Lactames
Síntesi asimètrica
Alkaloids
Lactams
Asymmetric synthesis
Descrição
Resumo:Starting from tricyclic lactam 2 , which is easily accessible by cyclocondensation of δ‐oxoester 1 with (R )‐phenylglycinol, a three‐step synthetic route to enantiopure 1‐substituted tetrahydroisoquinolines, including 1‐alkyl‐, 1‐aryl‐, and 1‐benzyltetrahydroisoquinoline alkaloids, as well as the tricyclic alkaloid (-)‐crispine A, has been developed. The key step is a stereoselective α‐amidoalkylation reaction using the appropriate Grignard reagent.