Enantioselective photocatalytic synthesis of bicyclo[2.1.1]hexanes as orthodisubstituted benzene bioisosteres with improved biological activity
Pablo Garrido-Garcia,
Irene Quiros,
Paula Milan-Rois
et al.
Abstract:1,5-Disubstituted bicyclo[2.1.1]hexanes are bridged scaffolds with well-defined exit vectors that are becoming increasingly popular building blocks in medicinal chemistry since they are saturated bioisosteres of orthosubstituted phenyl rings. Here we have developed the first enantioselective catalytic strategy based on a Lewis acid-catalyzed [2+2] photocycloaddition to obtain these motifs as enantioenriched scaffolds, providing an efficient approach for their incorporation in a variety of drug analogues. The b… Show more
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