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Palladium-Catalyzed Carbonylative Transformations of Bromhexine into Bioactive Compounds as Glucocerebrosidase Inhibitors



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.