Lesinurad, also known as RDEA594, is a selective uric acid re-absorption inhibitor (SURI) and is also a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body. RDEA594 has been shown to normalize the amount of uric acid excreted by gout patients previously classified as under-excretors. Lesinurad received FDA approval on December 22, 2015.
Lei X, Wang Y, Fan E, Sun Z. In Situ Activation of Disulfides for Multicomponent Reactions with Isocyanides and a Broad Range of Nucleophiles. Org Lett. 2019 Mar 1;21(5):1484-1487. doi: 10.1021/acs.orglett.9b00275. Epub 2019 Feb 11. PubMed PMID: 30740981.
Halama, Aleš & Stach, Jan & Rádl, Stanislav & Benediktová, Kristýna. (2018). Identification of an Unexpected Impurity in a New Improved Synthesis of Lesinurad. Organic Process Research & Development. 22. 10.1021/acs.oprd.8b00316.
Girardet, Jean-Luc; Koh, Yung-Hyo; De la Rosa, Martha; Gunic, Esmir; Hong, Zhi; Lang, Stanley; Kim, Hong Woo. Preparation of S-triazolyl α-mercaptoacetanilides as inhibitors of HIV reverse transcriptase. WO 2006026356. (Assignee Valeant Research & Development, USA)
Quart, Barry D.; Girardet, Jean-Luc; Gunic, Esmir; Yeh, Li-Tain. Preparation of azole carboxylates as modulators of blood uric acid levels. WO 2009070740. (Assignee Ardea Biosciences, Inc., USA)
Gunic, Esmir; Girardet, Jean-Luc; Vernier, Jean-Michel; Tedder, Martina E.; Paisner, David A.. Preparation of naphthalene thio triazole derivatives and their use for modulating uric acid levels. US 20100056465. (Assignee Ardea Biosciences, USA)
Gunic, Esmir; Girardet, Jean-Luc; Vernier, Jean-Michel; Tedder, Martina E.; Paisner, David A.. Preparation of naphthalene thio triazole derivatives and their use for modulating uric acid levels. US 20100056464. (Assignee Ardea Biosciences, USA)
Gunic, Esmir; Galvin, Gabriel. Manufacture of 2-[5-bromo-4-(cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio]acetic acid and related compounds. WO 2014008295. (Assignee Ardea Biosciences, Inc., USA)
Luo, Jian; Liu, Lixue; Rajeev, Kumar; Zhu, Wenmin; Li, Lei. Process for the purification of 2-[[5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl]thio]acetic acid. CN 104447589. (Assignee Sunshine Lake Pharma Co., Ltd., Peop. Rep. China)
Stach, Jan; Radl, Stanislav; Zvatora, Pavel; Pisa, Ondrej; Benediktova, Kristyna; Halama, Ales. Process for preparing 2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid. EP 3281941. (Assignee Zentiva K.S., Czech Rep.)
Bodhuri, Prabhudas; Green, Melanie R. A.; Karadeolian, Avedis; Weeratunga, Gamini; Gorin, Boris. Processes for the preparation of lesinurad and intermediates thereof. US 20180258057. (Assignee Apotex Inc., Can.)