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Keywords:

  • Cross-coupling;
  • Carbonylation;
  • Palladium;
  • Medicinal chemistry;
  • Inhibitors;
  • Biological activity

Abstract

A general synthesis for dicarbonylated derivatives of the parent drug bromhexine is described. By using the commercially available Pd(OAc)2/BuPAd2 (CataCXium A, Ad = adamantyl) catalyst system, the carbonylative arylation, amination, and alkoxylation of bromhexine proceeded with up to 79 % product yield. Selected synthesized derivatives of bromhexine showed improved effects as glucocerebrosidase inhibitors.