DNA-Conjugated Cyclopropane Derivatives Constructed from Sulfonium Ylides with α,β-Unsaturated Ketones

Bioconjug Chem. 2023 Sep 20;34(9):1523-1527. doi: 10.1021/acs.bioconjchem.3c00291. Epub 2023 Aug 17.

Abstract

Here, we report a DNA-compatible reaction for the generation of cyclopropane derivatives using thiolides with α,β-unsaturated ketones in the absence of transition metal and N2 protection, which is convenient for DNA encoded library (DEL) construction. This approach allows the rapid and efficient production of a series of DEL libraries of potentially biologically active cyclopropanes and spirocyclopropyl oxindole derivatives.

MeSH terms

  • Cloning, Molecular
  • Cyclopropanes*
  • DNA*
  • Ketones

Substances

  • cyclopropane
  • Cyclopropanes
  • DNA
  • Ketones