Expanding the diversity of purine libraries

Academic Article


  • In recent years, there has been a resurgence of interest in the synthesis of purine derivatives due to the discovery of purine-derived ligands for a variety of nucleotide dependent enzymes. The majority of chemistry has focused on substitution of the purine core structure by alkylation at N9 and nucleophilic-aromatic substitution reactions at C2 and C6. Here we report the syntheses of aryl, N-aryl, O-aryl substituted purine libraries by the palladium-mediated coupling of boronic acids, anilines or phenols at the C2 position, and copper(II)-mediated N-arylation with boronic acids at the N9 position. The chemistry described here greatly expands our ability to introduce different functionality and create new purine scaffolds. © 2001 Published by Elsevier Science Ltd.
  • Authors

    Digital Object Identifier (doi)

    Author List

  • Ding S; Gray NS; Ding Q; Schultz PG
  • Start Page

  • 8751
  • End Page

  • 8755
  • Volume

  • 42
  • Issue

  • 50