Qing Meng, Tong Zhao, Dongwei Kang, Boshi Huang, Peng Zhan, Xinyong Liu
{"title":"The development of an effective synthetic route of lesinurad (RDEA594).","authors":"Qing Meng, Tong Zhao, Dongwei Kang, Boshi Huang, Peng Zhan, Xinyong Liu","doi":"10.1186/s13065-017-0316-y","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Lesinurad is a novel selective uric acid salt transport protein 1 (URAT1) inhibitor which is approved in the USA for the treatment of gout. However, there are some shortcomings among the reported synthetic routes, such as expensive materials, environmental pollution and poor yield.</p><p><strong>Results: </strong>In this study, an efficient, practical and environmentally-friendly synthetic route of lesinurad is reported. The main advantages of this route include inexpensive starting materials, mild conditions and acceptable overall yield (38.8%).</p><p><strong>Conclusion: </strong>Generally, this procedure is reasonable, reliable and suitable for industrial production. Graphical abstract The improved synthetic procedure of lesinurad (I).</p>","PeriodicalId":9842,"journal":{"name":"Chemistry Central Journal","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2017-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1186/s13065-017-0316-y","citationCount":"7","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemistry Central Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1186/s13065-017-0316-y","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"Chemistry","Score":null,"Total":0}
引用次数: 7
Abstract
Background: Lesinurad is a novel selective uric acid salt transport protein 1 (URAT1) inhibitor which is approved in the USA for the treatment of gout. However, there are some shortcomings among the reported synthetic routes, such as expensive materials, environmental pollution and poor yield.
Results: In this study, an efficient, practical and environmentally-friendly synthetic route of lesinurad is reported. The main advantages of this route include inexpensive starting materials, mild conditions and acceptable overall yield (38.8%).
Conclusion: Generally, this procedure is reasonable, reliable and suitable for industrial production. Graphical abstract The improved synthetic procedure of lesinurad (I).
期刊介绍：
BMC Chemistry is an open access, peer reviewed journal that considers all articles in the broad field of chemistry, including research on fundamental concepts, new developments and the application of chemical sciences to broad range of research fields, industry, and other disciplines. It provides an inclusive platform for the dissemination and discussion of chemistry to aid the advancement of all areas of research.
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