Issue 13, 2022

Synthetic routes to bicyclo[1.1.1]pentylamines: booming toolkits for drug design

Abstract

With the flourishing progress of modern medicinal chemistry, bicyclo[1.1.1]pentylamines (BCPAs) have come to the fore as bioisosteres of arylamine motifs to reduce the growing concern about the risks of arylamines related to metabolism, bioavailability, and excretion. In light of the prevalence and significance of BCPAs, an increasing number of new practical protocols to efficiently furnish these appealing molecules have been thus disclosed, which serve to shorten the long synthetic sequences or enable gram-scale syntheses through one-pot multicomponent processes, creating a novel chemical space and systematically streamlining drug design routes.

Graphical abstract: Synthetic routes to bicyclo[1.1.1]pentylamines: booming toolkits for drug design

Article information

Article type
Highlight
Submitted
03 May 2022
Accepted
27 May 2022
First published
31 May 2022

Org. Chem. Front., 2022,9, 3591-3597

Synthetic routes to bicyclo[1.1.1]pentylamines: booming toolkits for drug design

Z. Yu and L. Shi, Org. Chem. Front., 2022, 9, 3591 DOI: 10.1039/D2QO00703G

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