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Strain-Release [2π + 2σ] Cycloadditions for the Synthesis of Bicyclo[2.1.1]hexanes Initiated by Energy Transfer
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2022-04-27 , DOI: 10.1021/jacs.2c02976
Renyu Guo 1 , Yu-Che Chang 1 , Loic Herter 2, 3 , Christophe Salome 2 , Sarah E Braley 1 , Thomas C Fessard 2 , M Kevin Brown 1
Affiliation  

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.

中文翻译:


由能量转移引发的应变释放 [2π + 2σ] 环加成合成双环[2.1.1]己烷



饱和自行车在新药物的设计和开发中变得越来越重要。这里描述了一种合成双环[2.1.1]己烷的新策略。这些自行车很重要,因为它们定义了退出向量,但许多替代模式作为构建块尚未得到充分探索。该过程涉及双环[1.1.0]丁烷的敏化,然后与烯烃进行环加成。讨论了该方法的范围和机制细节。
更新日期:2022-04-27
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