Multifunctional Building Blocks Compatible with Photoredox-Mediated Alkylation for DNA-Encoded Library Synthesis

Org Lett. 2020 Feb 7;22(3):1046-1051. doi: 10.1021/acs.orglett.9b04568. Epub 2020 Jan 15.

Abstract

DNA-encoded library (DEL) technology has emerged as a novel interrogation modality for ligand discovery in the pharmaceutical industry. Given the increasing demand for a higher proportion of C(sp3)-hybridized centers in DEL platforms, a photoredox-mediated cross-coupling and defluorinative alkylation process is introduced using commercially available alkyl bromides and structurally diverse α-silylamines. Notably, no protecting group strategies for amines are necessary for the incorporation of a variety of amino-acid-based organosilanes, providing crucial branching points for further derivatization.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alkylation
  • Amines / chemical synthesis*
  • Amines / chemistry
  • DNA / chemistry*
  • Hydrocarbons, Brominated / chemistry*
  • Molecular Structure
  • Oxidation-Reduction
  • Photochemical Processes
  • Stereoisomerism

Substances

  • Amines
  • Hydrocarbons, Brominated
  • DNA