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Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold

The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from β-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. The β...

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Detalles Bibliográficos
Autores principales: Blanco-Ania, Daniel, Valderas-Cortina, Carolina, Hermkens, Pedro H.H., Sliedregt, Leo A.J.M., Scheeren, Hans W., Rutjes, Floris P.J.T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6257290/
https://www.ncbi.nlm.nih.gov/pubmed/20428042
http://dx.doi.org/10.3390/molecules15042269
Descripción
Sumario:The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from β-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. The β-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenagel condensation reaction, a 1,3-dipolar cycloaddition reaction, and a nitrile reduction.