Rajarathnam E. Reddy, Casey J. Maguire, Riley H. Hastings, Timothy L’Hommedieu, Michael C. Dennis, Haiyan L. Grady, Srinivas Peddapatla, Michael A. Haley, II
{"title":"Review of the Synthesis of Timolol Maleate and Brimonidine Tartrate Drug Substances Used for the Treatment of Open-Angle Glaucoma","authors":"Rajarathnam E. Reddy, Casey J. Maguire, Riley H. Hastings, Timothy L’Hommedieu, Michael C. Dennis, Haiyan L. Grady, Srinivas Peddapatla, Michael A. Haley, II","doi":"10.1021/acs.oprd.4c00280","DOIUrl":null,"url":null,"abstract":"Open-angle glaucoma (OAG) is a chronic and degenerative disorder that causes optic nerve damage and potential blindness. The objective of this review is to provide a brief overview on OAG, with emphasis on the importance of β-blockers and α<sub>2</sub>-agonists for eye care. Timolol maleate (<b>1</b>) and brimonidine tartrate (<b>2</b>) are an important β-blocker and α<sub>2</sub>-agonist, respectively. Both are used in several medications for the treatment of open-angle glaucoma. A literature review of various synthetic approaches for timolol maleate (<b>1</b>), and brimonidine tartrate (<b>2</b>) drug substances is presented. In addition, the reported timolol maleate (<b>1</b>) and brimonidine tartrate (<b>2</b>) synthetic routes were assessed for strengths and weaknesses from a process chemistry perspective. A summary is provided based on drug substance quality, process, safety, and environmental considerations.","PeriodicalId":55,"journal":{"name":"Organic Process Research & Development","volume":"13 1","pages":""},"PeriodicalIF":3.5000,"publicationDate":"2025-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Organic Process Research & Development","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1021/acs.oprd.4c00280","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
引用次数: 0
Abstract
Open-angle glaucoma (OAG) is a chronic and degenerative disorder that causes optic nerve damage and potential blindness. The objective of this review is to provide a brief overview on OAG, with emphasis on the importance of β-blockers and α2-agonists for eye care. Timolol maleate (1) and brimonidine tartrate (2) are an important β-blocker and α2-agonist, respectively. Both are used in several medications for the treatment of open-angle glaucoma. A literature review of various synthetic approaches for timolol maleate (1), and brimonidine tartrate (2) drug substances is presented. In addition, the reported timolol maleate (1) and brimonidine tartrate (2) synthetic routes were assessed for strengths and weaknesses from a process chemistry perspective. A summary is provided based on drug substance quality, process, 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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