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Keywords:

  • guanidines;
  • heterocycles;
  • homogeneous catalysis;
  • isocyanides;
  • oxidation
Thumbnail image of graphical abstract

O2 in, H2O out: Various diamines and related bisnucleophiles readily undergo oxidative isocyanide insertion with Pd(OAc)2 (1 mol %) as the catalyst and O2 as the terminal oxidant to give a diverse array of medicinally relevant N heterocycles. The utility of this highly sustainable method is demonstrated by a formal synthesis of the antihistamines astemizole and norastemizole.