Palladium-Catalyzed Hydroxycarbonylation of (Hetero)aryl Halides for DNA-Encoded Chemical Library Synthesis

Bioconjug Chem. 2019 Aug 21;30(8):2209-2215. doi: 10.1021/acs.bioconjchem.9b00447. Epub 2019 Jul 31.


A strategy for DNA-compatible, palladium-catalyzed hydroxycarbonylation of (hetero)aryl halides on DNA-chemical conjugates has been developed. This method generally provided the corresponding carboxylic acids in moderate to very good conversions for (hetero)aryl iodides and bromides, and in poor to moderate conversions for (hetero)aryl chlorides. These conditions were further validated by application within a DNA-encoded chemical library synthesis and subsequent discovery of enriched features from the library in selection experiments against two protein targets.

Publication types

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

MeSH terms

  • Catalysis
  • DNA / chemistry*
  • Hydrocarbons, Halogenated / chemistry*
  • Palladium
  • Proteins / antagonists & inhibitors
  • Small Molecule Libraries / chemical synthesis*


  • Hydrocarbons, Halogenated
  • Proteins
  • Small Molecule Libraries
  • Palladium
  • DNA