1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho / meta -substituted arenes

作者：Jin‐Xin Zhao, Yuxuan Chang, Chi He, Benjamin J. Burke, Michael R. Collins, Matthew Del Bel, Jeff Elleraas, Gary M. Gallego, T. Patrick Montgomery, James J. Mousseau, Sajiv K. Nair, Matthew A. Perry, Jillian E. Spangler, Julien C. Vantourout, Phil S. Baran · 发表于：Proceedings of the National Academy of Sciences · 年份：2021 · DOI：10.1073/pnas.2108881118 · 被引用次数：123 · 研究领域：Catalytic C–H Functionalization Methods、Oxidative Organic Chemistry Reactions、Asymmetric Synthesis and Catalysis

Significance Bioisoteric replacements for aromatic rings to improve medicinal properties are in high demand. This work presents a comprehensive analysis of heretofore-inaccessible 1,2-difunctionalized bicyclo[1.1.1]pentanes from both chemical and biological vantage points. This analysis will aid those in drug discovery regarding when the application of such systems makes sense and how to access them in such circumstances.