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Exploring the Reactivity of Rigid 1-Azadienes Derived from Methylene γ-Lactams. Applications to the Stereoselective Synthesis of Spiro-γ-Lactams.
López-Francés, Adrián; Serna-Burgos, Zuriñe; Del Corte, Xabier; de Los Santos, Jesús M; de Cózar, Abel; Vicario, Javier.
Afiliación
  • López-Francés A; Department of Organic Chemistry I, Faculty of Pharmacy, University of the Basque Country, UPV/EHU. Paseo de la Universidad 7, Vitoria-Gasteiz 01006, Spain.
  • Serna-Burgos Z; Department of Organic Chemistry I, Faculty of Pharmacy, University of the Basque Country, UPV/EHU. Paseo de la Universidad 7, Vitoria-Gasteiz 01006, Spain.
  • Del Corte X; Department of Organic Chemistry I, Faculty of Pharmacy, University of the Basque Country, UPV/EHU. Paseo de la Universidad 7, Vitoria-Gasteiz 01006, Spain.
  • de Los Santos JM; Department of Organic Chemistry I, Faculty of Pharmacy, University of the Basque Country, UPV/EHU. Paseo de la Universidad 7, Vitoria-Gasteiz 01006, Spain.
  • de Cózar A; Department of Organic Chemistry I, Donostia International Physics Centre (DIPC), University of the Basque Country, UPV/EHU. Paseo Manuel de Lardizabal, 3, Donostia-San Sebastián 20018, Spain.
  • Vicario J; Ikerbasque, Basque Foundation for Science, Plaza Euskadi 5, Bilbao 48009, Spain.
J Org Chem ; 89(13): 9502-9515, 2024 Jul 05.
Article en En | MEDLINE | ID: mdl-38901015
ABSTRACT
A study on the reactivity of rigid 1-azadienes derived from methylene γ-lactams is reported. Through the functionalization of 1-amino α,ß-unsaturated γ-lactam derivatives, easily available from a multicomponent reaction of amines, aldehydes, and pyruvates, it is possible to in situ generate rigid 1-azadienes locked by a γ-lactam core. The 4π-electron system of those rigid 1-azadienes can behave as both diene and dienophile species through a spontaneous cyclodimerization reaction or exclusively as dienes or dienophiles if they are trapped with imines or cyclopentadiene, respectively. The use of chiral rigid 1-azadienes as dienophiles in the cycloaddition reaction with cyclopentadiene leads to the formation of spiro-γ-lactams bearing four stereogenic centers in a highly stereospecific manner, reporting the first example of the use of methylene-γ-lactams in the synthesis of spirocycles.

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Org Chem Año: 2024 Tipo del documento: Article País de afiliación: España Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: J Org Chem Año: 2024 Tipo del documento: Article País de afiliación: España Pais de publicación: Estados Unidos