螺旋桨烷
激进的
电泳剂
化学
组合化学
亲核细胞
芳基
亲电取代
材料化学
计算化学
烷基
有机化学
双环分子
分子
催化作用
绿色化学
超分子化学
作者
Weichen Huang,Sebastian Keeß,Gary A. Molander
标识
DOI:10.1002/anie.202302223
摘要
1-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.
科研通智能强力驱动
Strongly Powered by AbleSci AI