Abstract
BackgroundLesinurad 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.ResultsIn 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%).ConclusionGenerally, this procedure is reasonable, reliable and suitable for industrial production.Graphical abstractThe improved synthetic procedure of lesinurad (I).
Highlights
Lesinurad is a novel selective uric acid salt transport protein 1 (URAT1) inhibitor which is approved in the USA for the treatment of gout
Sustained hyperuricemia is the most important biochemical basis of gout: normal adults produce about 750 mg of uric acid every day, of which approximately two-thirds of total urate is endogenous, while the remaining is from dietary purines
Several research-scale synthetic methods have been reported for the preparation of Lesinurad (Schemes 1, 2, 3 and 4), which were associated with several drawbacks, such as the expensive materials, usage of hazardous reagents and poor yields [14, 15]
Summary
Lesinurad is a novel selective uric acid salt transport protein 1 (URAT1) inhibitor which is approved in the USA for the treatment of gout. Several research-scale synthetic methods have been reported for the preparation of Lesinurad (Schemes 1, 2, 3 and 4), which were associated with several drawbacks, such as the expensive materials, usage of hazardous reagents and poor yields [14, 15]. Both two routes are not practically valuable because of the commercially unavailable starting material, the long reaction time and low overall yield [20].
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