Abstract1‐Aryl‐substituted bicyclo[1.1.1]pentanes (BCPs) are an important class of BCP derivatives with widespread application in drug development. Most syntheses of these materials require multiple chemical steps via BCP electrophiles or nucleophiles derived from [1.1.1]propellane. Although one‐step, multicomponent radical cross‐coupling reactions could provide a more sustainable and rapid route to access diverse heteroarylated BCPs, current approaches are limited to tertiary alkyl radicals, leading to a decrease in their practical value. In this study, a conceptually different approach enabled by a radical multicomponent heteroarylation of [1.1.1]propellane to access functionalized heteroarylated BCPs is described. Importantly, this protocol is compatible with primary‐, secondary‐, and tertiary aliphatic radicals, as well as various fluoroalkyl radical sources, thus enabling rapid library generation of sought‐after BCP derivatives for drug development.

中文翻译：

---

通过[1.1.1]丙烷光催化多组分杂芳基化实现功能化双环[1.1.1]戊烷杂芳基的通用且实用的路线

摘要1-芳基取代的双环[1.1.1]戊烷（BCP）是一类重要的BCP衍生物，在药物开发中广泛应用。这些材料的大多数合成需要通过 BCP 亲电子试剂或源自 [1.1.1]丙烷的亲核试剂进行多个化学步骤。虽然一步、多组分自由基交叉偶联反应可以提供一种更可持续、更快速的途径来获得多种杂芳基化 BCP，但目前的方法仅限于叔烷基，导致其实用价值下降。在这项研究中，描述了一种概念上不同的方法，通过[1.1.1]丙烷的自由基多组分杂芳基化来获得功能化的杂芳基化 BCP。重要的是，该方案与一级、二级和三级脂肪族自由基以及各种氟烷基自由基来源兼容，从而能够快速生成用于药物开发的广受欢迎的 BCP 衍生物的库。