Yb(OTf)3-Catalyzed [2π + 2σ] Cycloaddition of Bicyclo[1.1.0]butanes with Methylenimines for Modular Synthesis of 1,2,4-Trisubstituted 2-Aza-bicyclo[2.1.1]hexanes
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Aromatic rings in drug candidates often exhibit poor developability. Three-dimensional bioisosteres like aza-bicyclo[2.1.1]hexanes (aza-BCHs) improve properties but face limited synthetic access to diverse substitutions. Herein, we report a Yb(OTf)3-catalyzed ... ...
