Stereoselective polysubstituted bicyclo[1.1.0]butane synthesis by rhodium-catalyzed kinetic resolution.

Rhodium-catalyzed kinetic resolution enables stereoselective synthesis of highly enantioenriched polysubstituted bicyclo[1.1.0]butanes with broad substrate scope.

• Why it matters: The enantioselective synthesis of polysubstituted BCBs remains a significant challenge in synthetic chemistry, limiting their application in medicinal chemistry and complex molecule construction.
• What they did: A general platform was developed using chiral dirhodium catalysts and triftosylhydrazones to perform stepwise or one-pot cycloaddition reactions, producing chiral or meso 1,2,3,4-tetrasubstituted BCBs.
• The result: The catalyst Rh 2 ( R -3,5- di PheTPCP) 4 achieves high enantioselectivity through kinetic resolution, operating under mild conditions with readily available materials, expanding access to complex BCB derivatives.