Molecules (Apr 2024)

Skeletal Editing: Ring Insertion for Direct Access to Heterocycles

  • Xue Li,
  • Zhigang Xu

DOI
https://doi.org/10.3390/molecules29091920
Journal volume & issue
Vol. 29, no. 9
p. 1920

Abstract

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Skeleton editing has rapidly advanced as a synthetic methodology in recent years, significantly streamlining the synthesis process and gaining widespread acceptance in drug synthesis and development. This field encompasses diverse ring reactions, many of which exhibit immense potential in skeleton editing, facilitating the generation of novel ring skeletons. Notably, reactions that involve the cleavage of two distinct rings followed by the reformation of new rings through ring insertion play a pivotal role in the construction of novel ring skeletons. This article aims to compile and systematize this category of reactions, emphasizing the two primary reaction types and offering a thorough exploration of their associated complexities and challenges. Our endeavor is to furnish readers with comprehensive reaction strategies, igniting research interest and injecting fresh impetus into the advancement of this domain.

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