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April 30, 2026Journal of the American Chemical Society4 citationsOpen Access

Asymmetric Synthesis of S -Trifluoromethyl Sulfoxide and Sulfoximine Pharmacophores

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NKNa Yeon KwonJYJustin YeJEJonathan A. Ellman

Key Points

  • To explore and optimize the asymmetric synthesis of S-trifluoromethyl sulfoxide and sulfoximine pharmacophores.
  • Cleavage of acyl group to form free-NH sulfilimine
  • Hydrolysis via backside displacement of amine resulting in sulfoxide formation
  • Inversion of stereochemistry observed during the synthesis.
  • Successful synthesis of S-trifluoromethyl sulfoxide with clear stereochemical inversion.
  • Formation of sulfoximine linked to hydrolysis of sulfilimine.
  • Novel pathways identified for potential drug development.

Abstract

-acyl group is first cleaved to give the free-NH sulfilimine that then undergoes hydrolysis by backside displacement of the amine to give the sulfoxide with inversion of stereochemistry.

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Cite This Study

Kwon et al. (2026) studied this question.

synapsesocial.com/papers/69f2f0991e5f7920c6386c69https://doi.org/10.1021/jacs.6c03062
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