The development of an effective synthetic route of lesinurad (RDEA594)
Qing Meng1, Tong Zhao1, Dongwei Kang1
1Department 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.
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).
