SuFExable NH-Pyrazoles via 1,3-Dipolar Cycloadditions of Diazo Compounds with Bromoethenylsulfonyl Fluoride

J Org Chem. 2022 Mar 4;87(5):3868-3873. doi: 10.1021/acs.joc.1c03105. Epub 2022 Feb 10.

Abstract

"Click" reactions have transformed the molecular sciences. Augmenting cycloaddition reactions, sulfur(VI) fluoride exchange (SuFEx) chemistry has diversified the landscape of molecular assembly. Herein, we report a facile strategy to access SuFExable NH-pyrazoles via strain and catalyst-free 1,3-dipolar cycloadditions of stabilized diazo compounds under mild conditions. Subsequent SuFEx proceeds efficiently with various N- and O-nucleophiles. Access to SuFExable NH-pyrazoles─a class of compounds containing two common pharmacophores─enables future opportunities within drug discovery, chemical biology, materials chemistry, and related fields.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azo Compounds
  • Click Chemistry
  • Cycloaddition Reaction
  • Fluorides* / chemistry
  • Pyrazoles*
  • Sulfur / chemistry

Substances

  • Azo Compounds
  • Pyrazoles
  • Sulfur
  • Fluorides