Synthesis and characterization of nebivolol: a review of different synthetic approaches and their efficiencies

Abstract

Nebivolol is a potent beta-blocker used to treat heart failure and hypertension. With the increasing prevalence of cardiovascular diseases and the demand for effective and well-tolerated treatments, the global market for beta-blockers, including nebivolol, was worth approximately US$8.5 billion in 2020 and is projected to grow by 5.5% in the coming years. There are several techniques for synthesizing nebivolol, including Sharpless asymmetric epoxidation, Pd-, Zr-, and Mo-catalyzed processes, photochemical reconfiguration, and homochiral sulfoxide-directed reaction (Jiang et al., 2021). Among these techniques, Zr- and Mo-catalyzed processes produce the highest efficiency of 99%. However, using natural chiral starting materials and Sharpless asymmetric epoxidation is more efficient in terms of time and cost. This review article provides an in-depth analysis of the effectiveness of the various nebivolol synthesis techniques. The commercial expansion of beta-blockers and the rising need for efficient and well-tolerated medicines emphasize how critical it is to conduct further research in this area.