Unlocking congested 3D molecul... Note

Unlocking congested 3D molecular architectures for drug discovery

A strategy is developed that merges triplet nitrene-mediated ring expansion with titanium-catalysed cyanylation for the diastereoselective synthesis of vicinal tetrasubstituted cyclobutane amino nitriles. This strategy unlocks highly functionalized and congested three-dimensional cyclobutanes that could provide scaffolds for drug discovery but have previously been difficult to access.