Molecular diversity by olefin cross-metathesis on solid support. Generation of libraries of biologically promising β-lactam derivatives

The application of the reagent-based diversification strategy for generation of libraries of biologically promising β-lactam derivatives is described. Key features are the versatility of the linker used and the cross-metathesis functionalization at the cleavage step. From an immobilized primary libr...

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Detalhes bibliográficos
Autores: Mendez, Luciana, Poeylaut Palena, Andrés Alberto, Mata, Ernesto Gabino
Formato: artículo
Estado:Versión publicada
Fecha de publicación:2018
País:Argentina
Recursos:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/87280
Acesso em linha:http://hdl.handle.net/11336/87280
Access Level:acceso abierto
Palavra-chave:CHOLESTEROL ABSORPTION INHIBITORS
DIVERSITY ORIENTED SYNTHESIS
OLEFIN METATHESIS
SOLID-PHASE ORGANIC SYNTHESIS
Β-LACTAM DERIVATIVES
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
Descrição
Resumo:The application of the reagent-based diversification strategy for generation of libraries of biologically promising β-lactam derivatives is described. Key features are the versatility of the linker used and the cross-metathesis functionalization at the cleavage step. From an immobilized primary library, diversity was expanded by applying different cleavage conditions, leading to a series of cholesterol absorption inhibitor analogues together with interesting hybrid compounds through incorporation of a chalcone moiety.