On-DNA Synthesis of 2-Hydroxy Dithiocarbamates

Org Lett. 2025 Nov 21;27(46):12840-12845. doi: 10.1021/acs.orglett.5c04222. Epub 2025 Nov 6.

Abstract

We present a modular on-DNA bridging strategy that addresses key reactivity challenges in DNA-encoded library synthesis. By generation of a reactive carbamodithioic acid intermediate from secondary amines, this method enables efficient coupling with epoxides to produce diverse 2-hydroxy dithiocarbamate scaffolds. Gentle and DNA-compatible, it offers a versatile platform for rapid, structurally diverse DEL construction with significant drug discovery potential.

MeSH terms

  • Amines / chemistry
  • DNA* / chemistry
  • Epoxy Compounds / chemistry
  • Molecular Structure
  • Thiocarbamates* / chemical synthesis
  • Thiocarbamates* / chemistry

Substances

  • DNA
  • Thiocarbamates
  • Amines
  • Epoxy Compounds