2,5-disubstituted bicyclo[2.1.1]hexanes as rigidified cyclopentane variants

Identification of rigid counterparts for common flexible scaffolds is crucial to the advancement of medicinal chemistry. Here we showcase a new class of building blocks, 2,5-disubstituted bicyclo[2.1.1]hexanes that can act as rigidified cis-, or trans-1,3-disubstituted cyclopentanes, common motifs i...

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Detalles Bibliográficos
Autores principales: Paul, Shashwati, Adelfinsky, Daniel, Salome, Christophe, Fessard, Thomas, Brown, M. Kevin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2023
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10395266/
https://www.ncbi.nlm.nih.gov/pubmed/37538817
http://dx.doi.org/10.1039/d3sc02695g
Descripción
Sumario:Identification of rigid counterparts for common flexible scaffolds is crucial to the advancement of medicinal chemistry. Here we showcase a new class of building blocks, 2,5-disubstituted bicyclo[2.1.1]hexanes that can act as rigidified cis-, or trans-1,3-disubstituted cyclopentanes, common motifs in drugs. The scalable synthesis of these structures was enabled through the use of C–H functionalization logic and cycloaddition reactions.

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