Nature | Chemistry
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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.