Background: Spiro skeleton is an important structural motif in natural products, usually accounting
for their formidable architectures and remarkable biological profiles. Recent advances demonstrated that a diverse
range of scenarios held the promise for the assembly of spirocenter based on ortho-dearomatization strategy.
In this article, we describe the latest development of ortho-dearomatization reaction in constructing spirocyclic
scaffolds with an all-carbon ring junction from a methodological standpoint.
Objective: The review focuses on recent progress in the area of ortho-dearomatization reaction in constructing
spirocyclic scaffolds with an all-carbon ring junction.
Conclusion: In summary, we have summarized the capability of ortho-dearomatization reaction to construct
spirocyclic skeleton, a common structural pattern found at the core of numerous natural products with broad
structural diversities and important bioactivities. Success in this area will benefit not only the area of synthetic
chemistry through methodological development, but also medicinal chemistry and chemical biology by providing
access to rapid assembly of bioactive compounds’ core scaffolds.