Rajarathnam E. Reddy*, Alexander S. Wong, David J. Babinski and Michael A. Haley,
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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.
期刊介绍：
The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.
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