Pang Qiwen, Li Yang, Xie Xin, Tang Jie, Liu Qian, Peng Cheng, Li Xiang, Han Bo
State Key Laboratory of Southwestern Chinese Medicine Resources, Hospital of Chengdu University of Traditional Chinese Medicine, School of Pharmacy and College of Medical Technology, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Front Chem. 2022 Oct 21;10:997944. doi: 10.3389/fchem.2022.997944. eCollection 2022.
Bicyclo[1.1.1]pentylamines (BPCAs), emerging as sp-rich surrogates for aniline and its derivatives, demonstrate unique structural features and physicochemical profiles in medicinal and synthetic chemistry. In recent years, compared with conventional synthetic approaches, the rapid development of radical chemistry enables the assembly of valuable bicyclo[1.1.1]pentylamines scaffold directly through the amination transformation of highly strained [1.1.1]propellane. In this review, we concisely summarize the emerging role of radical chemistry in the construction of BCPAs motif, highlighting two different and powerful radical-involved strategies including -centered and -centered radical pathways under appropriate conditions. The future direction concerning BCPAs is also discussed at the end of this review, which aims to provide some inspiration for the research of this promising project.
双环[1.1.1]戊胺（BPCAs）作为苯胺及其衍生物中富含sp的替代物而崭露头角，在药物化学和合成化学中展现出独特的结构特征和物理化学性质。近年来，与传统合成方法相比，自由基化学的快速发展使得通过高张力[1.1.1]螺桨烷的胺化转化直接构建有价值的双环[1.1.1]戊胺骨架成为可能。在这篇综述中，我们简要总结了自由基化学在构建BCPAs基序中的新兴作用，重点介绍了两种不同且强大的涉及自由基的策略，包括在适当条件下的 - 中心和 - 中心自由基途径。本文末尾还讨论了关于BCPAs的未来方向，旨在为这个有前景的项目的研究提供一些启发。
