雷西纳德（RDEA594）有效合成路线的开发。
The development of an effective synthetic route of lesinurad (RDEA594).
作者信息
Meng Qing, Zhao Tong, Kang Dongwei, Huang Boshi, Zhan Peng, Liu Xinyong
机构信息
Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, No. 44 West Culture Road, Jinan, 250012, Shandong, People's Republic of China.
出版信息
Chem Cent J. 2017 Sep 5;11(1):86. doi: 10.1186/s13065-017-0316-y.
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).
背景
雷西纳德是一种新型的选择性尿酸盐转运蛋白1（URAT1）抑制剂，已在美国获批用于治疗痛风。然而，已报道的合成路线存在一些缺点，如原料昂贵、环境污染和产率低。
结果
本研究报道了一种高效、实用且环保的雷西纳德合成路线。该路线的主要优点包括起始原料廉价、条件温和且总产率可接受（38.8%）。
结论
总体而言，该方法合理、可靠且适合工业化生产。图摘要 雷西纳德（I）的改进合成方法。
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