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Keywords:

  • antitumor agents;
  • arylamination;
  • cross-coupling;
  • nucleosides;
  • palladium
Thumbnail image of graphical abstract

A mixed-ligand system of Pd/Synphos/Xantphos promotes effective C[BOND]N coupling in the synthesis of various N-arylaminotriazole and N-arylaminopurine nucleoside analogues. This catalytic system is strikingly powerful and efficient, allowing for unparalleled substrate scope and high product yields as well as promotion of C[BOND]Cl bond activation for C[BOND]N coupling. 31P NMR investigations provided useful evidence favoring a mechanism in which the catalytic reactions are mediated by ligand exchange during both Pd catalyst formation and oxidative insertion. For more details see the Communication by L. Peng et al. on page 2221 ff.