Synthesis of Active Metabolites of Carvedilol, an Antihypertensive Drug

Abstract

A simple synthetic route for active metabolites of carvedilol is reported. The metabolites 4′-hydroxycarvedilol and 5′-hydroxycarvedilol have exhibited high activity for β-blockade. We have disclosed syntheses of 4′-hydroxycarvedilol and 5′-hydroxycarvedilol from commercially available vanillin and isovanillin, respectively.

Keywords:

• Angina
• antihypertension
• carvedilol
• congestive heart failure
• metabolite
• 4-oxiranylmethoxy-9H-carbazole

ACKNOWLEDGMENTS

The authors thank Aurobindo Pharma Ltd. for supporting this work. The authors are also thankful to colleagues at the analytical research department and chemical research department of Aurobindo Research Center for the cooperation and fruitful discussions.