Published in
National Academy of Sciences, Proceedings of the National Academy of Sciences, 28(118), 2021
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1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho / meta -substituted arenes
Journal article published in 2021 by
Jin-Xin Zhao 
,
Yu-Xuan 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
,
Yu-Xuan 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
This paper is made freely available by the publisher.
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Abstract
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.