Preparation method of gout treatment drug Lesinurad and Lesinurad intermediate

Abstract

Provided are a novel Lesinurad intermediate, providing a synthetic process more economical, more efficient, safer, more environmentally friendly, and suitable for large-scale industrial production for the preparation of Lesinurad. Also provided is a method for preparing the known Lesinurad intermediate and Lesinurad via the provided novel Lesinurad intermediate. Using the novel Lesinurad intermediate of the present invention to synthesize Lesinurad has the following advantages of using cheap and easily available required raw materials, avoiding the use of heavy metals and solvents harmful to the environment, easily separating and purifying the intermediate and the product with a simple operation, avoiding the use of the thiophosgene having high toxicity and difficulty of operation, and enabling the total yield of the reaction to reach a level equal to or higher than the prior art.

Description

technical field

[0001] The invention relates to a preparation method of Lesinurad, a drug for treating gout, and a key intermediate thereof. Background technique

[0002] Gout is a crystal-associated arthropathy caused by deposition of monosodium urate (MSU), which is directly related to hyperuricemia caused by disturbance of purine metabolism and / or decreased uric acid excretion. There are more than 20 million gout patients worldwide. Lesinurad (RDEA594) is an oral uricosuric agent that inhibits the renal proximal tubule uric acid transporter URAT1. Previous exploratory studies in gout patients have shown that allopurinol (ALLO), combined with lesinurad, can reduce serum uric acid (SUA) more effectively than ALLO alone. Through the study of more than 500 healthy people and gout patients, it was found that Lesinurad reduced blood uric acid in a dose-dependent manner, and Febuxostat was well tolerated. It is also a xanthine oxidase inhibitor approved for the treatment of h...

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