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February 14, 2026Organic Letters0 citations

Carbon Atom Deletion Strategy Enabled Synthesis of 22- epi -6-Deoxocastasterone Using the Intact Skeleton of Tigogenin

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ZSZhi‐Hao ShangXLXiaodong LiDYDihua Yan

Key Points

  • This research aims to develop a carbon atom deletion strategy to synthesize 22-epi-6-deoxocastasterone from steroidal sapogenins.
  • Stepwise carbon atom deletion using oxidation, rearrangement, and borylation.
  • Conversion of C25 chiral methyl to C24 methyl.
  • Spiroketal ring-opening and one-pot deoxygenation transformations.
  • Successfully synthesized 22-epi-6-deoxocastasterone from natural precursors.
  • Demonstrated high atom economy in synthetic processes.
  • Provided a novel route for structural diversification of brassinosteroids.

Abstract

A stepwise carbon atom deletion strategy was developed to construct the brassinosteroid-type side chain from intact steroidal sapogenins with high atom economy. Key C23 deletion via oxidation, Favorskii rearrangement, and decarboxylative borylation converted the inherent C25 chiral methyl into the target C24 methyl. Further transformations, including spiroketal ring-opening and one-pot Barton-McCombie deoxygenation, enabled the efficient synthesis of a non-natural analogue, 22-epi-6-deoxocastasterone, offering a novel route for structural diversification.

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Cite This Study

Shang et al. (2026) studied this question.

synapsesocial.com/papers/699011712ccff479cfe5821bhttps://doi.org/10.1021/acs.orglett.6c00114
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