The incorporation of saturated bioisosteres of phenyl rings has emerged as an appealing strategy in drug-discovery programmes. However, stereocontrolled access to these sp3-hybridized skeletons remains elusive. Now, the enantioselective synthesis of bicyclo[2.1.1]hexanes has been achieved through a Lewis-acid-catalysed [2 + 2] photocycloaddition, making it possible to obtain different drug analogues with improved properties.
- Pablo Garrido-García
- Irene Quirós
- Mariola Tortosa