Synthesis of potential drug metabolites by a modified Udenfriend reaction

• Published in: Tetrahedron letters Vol. 52; no. 7; pp. 749 - 752
• Main Authors: Slavik, Roger, Peters, Jens-Uwe, Giger, Rudolf, Bürkler, Markus, Bald, Eric
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 16.02.2011; Elsevier
• Subjects: Accessibility; Aromatic hydroxylation; Biomedical materials; Biomimetic oxidation; chemical structure; Chemistry; Chemistry, Organic; chlorpromazine; derivatization; Diltiazem; Drug discovery; Drugs; hydroxylation; In vivo testing; In vivo tests; Metabolites; oxidation; Physical Sciences; propranolol; Science & Technology; Synthesis (chemistry); Aromatic hydroxylation; Drug discovery; Metabolites; Biomimetic oxidation; CLOZAPINE; RAT; DEMETHYLATION; MIST; HYDROGEN-PEROXIDE; FENTON REAGENT; MODEL; SELECTIVITY

The scope and the limitations of a modified Udenfriend reaction for the one-step synthesis of potential drug metabolites were explored. Several drugs (clozapine, chlorpromazine, imipramine, buspirone, diltiazem, and propranolol) were subjected to modified Udenfriend conditions (Fe 2+/Mn 2+/EDTA/asco...