A multi-substrate screening approach for the identification of a broadly applicable Diels-Alder catalyst

When developing a synthetic methodology, chemists generally optimize a single substrate and then explore the substrate scope of their method. This approach has led to innumerable and widely-used chemical reactions. However, it frequently provides methods that only work on model substrate-like compou...

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Detalles Bibliográficos
Autores: Kim, Hyejin, Gerosa, Gabriela Guillermina, Aronow, Jonas, Kasaplar, Pinar, Ouyang, Jie, Lingnau, Julia B., Guerry, Paul, Farès, Christophe, List, Benjamin
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2019
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/104577
Acceso en línea:http://hdl.handle.net/11336/104577
Access Level:acceso abierto
Palabra clave:ORGANOCATALYSIS
ASYMMETRIC SYNTHESIS
COMBINATORIAL LIBRARIES
https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
Descripción
Sumario:When developing a synthetic methodology, chemists generally optimize a single substrate and then explore the substrate scope of their method. This approach has led to innumerable and widely-used chemical reactions. However, it frequently provides methods that only work on model substrate-like compounds. Perhaps worse, reaction conditions that would enable the conversion of other substrates may be missed. We now show that a different approach, originally proposed by Kagan, in which a collection of structurally distinct substrates are evaluated in a single reaction vessel, can not only provide information on the substrate scope at a much earlier stage in methodology development, but even lead to a broadly applicable synthetic methodology. Using this multi-substrate screening approach, we have identified an efficient and stereoselective imidodiphosphorimidate organocatalyst for scalable Diels?Alder reactions of cyclopentadiene with different classes of α,β-unsaturated aldehydes.