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<p>Sulfonimidamides play an increasingly significant role in medicinal chemistry. However, the scarcity of efficient asymmetric methods has constrained their widespread applications. Herein, we report a simplified carbene-catalyzed <i>N</i>-acylation approach for the rapid synthesis of chiral unprotected acyclic SIAs. This transformation proceeds via a critical tautomerization process, affording a wide range of SIAs in good yield and with high enantioselectivities.</p>

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Enantioselective assembly of chiral acyclic sulfonimidamides via carbene-catalyzed desymmetric N-acylation

  • 期刊论文

  • 发表日期：

    2026年4月9日

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  • Yani Li,
  • Tianyi Wang,
  • Jian Wang

摘要

Sulfonimidamides play an increasingly significant role in medicinal chemistry. However, the scarcity of efficient asymmetric methods has constrained their widespread applications. Herein, we report a simplified carbene-catalyzed N-acylation approach for the rapid synthesis of chiral unprotected acyclic SIAs. This transformation proceeds via a critical tautomerization process, affording a wide range of SIAs in good yield and with high enantioselectivities.