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    Saturated bicycles are becoming ever more important in the design and development of new pharmaceuticals. Here a new strategy for the synthesis of bicyclo[2.1.1]hexanes is described. These bicycles are significant because they have defined exit vectors, yet many substitution patterns are underexplored as building blocks. The process involves sensitization of a bicyclo[1.1.0]butane followed by cycloaddition with an alkene. The scope and mechanistic details of the method are discussed.


    Renyu Guo, Yu-Che Chang, Loic Herter, Christophe Salome, Sarah E Braley, Thomas C Fessard, M Kevin Brown. Strain-Release [2π + 2σ] Cycloadditions for the Synthesis of Bicyclo[2.1.1]hexanes Initiated by Energy Transfer. Journal of the American Chemical Society. 2022 May 11;144(18):7988-7994

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    PMID: 35476547

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