Herein we report the decarboxylative Minisci heteroarylation of bicyclo[1.1.1]pentane (BCP) derivatives at the C2 (bridge) position. The developed process directly couples free BCP C2-carboxylic acids with non-prefunctionalised heteroarenes to provide rare examples of polysubstituted BCPs in synthetically useful yields. An extension of the methodology to the related 2-oxa-bicyclo[2.1.1]hexane motif was also achieved. Finally, the impact of the BCP core on the physicochemical properties of a representative example compared to its all-aromatic ortho- and meta-substituted analogues was evaluated.

中文翻译：

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双环[1.1.1]戊烷衍生物的桥杂芳基化

在这里，我们报告了双环 [1.1.1] 戊烷 (BCP) 衍生物在 C2（桥）位置的脱羧 Minisci 杂芳基化。开发的工艺直接将游离的 BCP C2-羧酸与非预官能化的杂芳烃偶联，以提供罕见的多取代 BCP 实例，其合成有用的产率。还实现了将方法扩展到相关的 2-oxa-bicyclo[2.1.1]hexane 基序。最后，评估了 BCP 核与其全芳邻位和间位取代类似物相比，对代表性示例的理化性质的影响。