Home Products Cited in Publications Worldwide 2,5-Disubstituted Bicyclo[2.1.1]hexanes as Rigidified Cyclopentane Variants for Medicinal Chemistry
Chem. Sci.,2023,14(30):8070-8075.
Shashwati Paul; Daniel Adelfinsky; Christophe Salome; Thomas Fessard; M. Kevin Brown
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.