Review of the Synthesis of Gatifloxacin and Ofloxacin Drug Substances Used for the Treatment of Eye Infections

A variety of eye infections are caused by microorganisms such as bacteria, viruses, fungi, and parasites, and they have a significant impact on eyes in all ages of population worldwide ranging from inconvenience, visual impairment, blindness, and death. The objective of this review is to provide a brief overview of eye infectious diseases, with an emphasis on the importance of quinolone antibiotics in eye care. Gatifloxacin (1) and ofloxacin (2) are important anti-infectious agents widely used for the treatment of ocular infections. A literature review of various synthetic approaches for the preparation of gatifloxacin (1) and ofloxacin (2) drug substances is presented. In addition, the reported gatifloxacin (1) and ofloxacin (2) synthetic routes were assessed for their strengths and weaknesses from a process chemistry perspective. A comparative summary is provided based on drug substance batch size, quality, process and manufacturability, safety, and environmental considerations.