The development of an effective synthetic route of lesinurad (RDEA594).

Q1 Chemistry Chemistry Central Journal Pub Date : 2017-09-05 DOI:10.1186/s13065-017-0316-y
Qing Meng, Tong Zhao, Dongwei Kang, Boshi Huang, Peng Zhan, Xinyong Liu
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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).

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一种有效合成莱辛努拉德(RDEA594)路线的建立。
背景:Lesinurad是一种新型的选择性尿酸盐转运蛋白1 (URAT1)抑制剂,在美国被批准用于治疗痛风。然而,目前报道的合成路线存在材料昂贵、环境污染和产率低等缺点。结果:本研究报道了一条高效、实用、环保的合成途径。该工艺的主要优点是原料便宜,条件温和,总产率可接受(38.8%)。结论:该工艺流程合理、可靠,适合工业化生产。图摘要:改进的lesinurad (I)合成工艺。
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来源期刊
Chemistry Central Journal
Chemistry Central Journal 化学-化学综合
CiteScore
4.40
自引率
0.00%
发文量
0
审稿时长
3.5 months
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. Sections: -Analytical Chemistry -Organic Chemistry -Environmental and Energy Chemistry -Agricultural and Food Chemistry -Inorganic Chemistry -Medicinal Chemistry -Physical Chemistry -Materials and Macromolecular Chemistry -Green and Sustainable Chemistry
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