A method of synthesizing the main metabolites of albendazole (albendazole-sulphoxide, albendazole sulphone and amino-albendazole-sulphone) is described. Synthesis of the three metabolites was obtained by subjecting raw albendazole to a series of chemical procedures. Albendazole-sulphoxide was obtained by oxidation of albendazole with NaIO4 in H2O/MeOH at room temperature: albendazole-sulphone was obtained by oxidation of albendazole with 30% H2O2 at 55°C: amino-albendazole-sulphone was obtained by hydrolysis with 15% KOH in EtOH/H2O by refluxing (scheme 1). In order to verify the identification of the metabolites obtained, NMR IR and HPLC analyses were carried out.
A new synthetic method of the main albendazole metabolites
De Laurentis N.;Crescenzo G.;
1996-01-01
Abstract
A method of synthesizing the main metabolites of albendazole (albendazole-sulphoxide, albendazole sulphone and amino-albendazole-sulphone) is described. Synthesis of the three metabolites was obtained by subjecting raw albendazole to a series of chemical procedures. Albendazole-sulphoxide was obtained by oxidation of albendazole with NaIO4 in H2O/MeOH at room temperature: albendazole-sulphone was obtained by oxidation of albendazole with 30% H2O2 at 55°C: amino-albendazole-sulphone was obtained by hydrolysis with 15% KOH in EtOH/H2O by refluxing (scheme 1). In order to verify the identification of the metabolites obtained, NMR IR and HPLC analyses were carried out.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
