Continuous flow synthesis of the URAT1 inhibitor lesinurad
Literature Information
Mariana C. F. C. B. Damião, Henrique M. Marçon, Julio Cezar Pastre
Herein, the urate anion exchange transporter 1 (URAT1) inhibitor lesinurad is synthesized from commercially available building blocks by a five-step linear continuous flow sequence. Our previously developed continuous flow platform was successfully applied to generate the 3-thio-1,2,4-triazole key intermediate 2 in 88% yield, after 55 minutes of residence time. Condensation, cyclization and S-alkylation were telescoped in a single operation without conducting solvent exchanges and intermediate purifications. Next, 1,2,4-triazole bromination and ester hydrolysis were also performed in continuous flow regime to deliver lesinurad in 68% overall yield in a total residence time of 2 hours. Our approach enables the fast generation of lesinurad and can be directly applied to produce major quantities of this important API.
Related Literature
Photoinduced asymmetric charge trapping in a symmetric tetraazapyrene-fused bis(tetrathiafulvalene) conjugate
Ping Zhou, Maryam Nazari Haghighi Pashaki, Hans-Martin Frey, Andreas Hauser, Silvio Decurtins, Andrea Cannizzo, Thomas Feurer, Robert Häner, Shi-Xia Liu
DOI: 10.1039/D3SC03184E
Nucleic acid degradation as barrier to gene delivery: a guide to understand and overcome nuclease activity
DOI: 10.1039/D3CS00194F
Interfacial engineering of transition metal dichalcogenide/carbon heterostructures for electrochemical energy applications
Fang He, Shi-Zhang Qiao
DOI: 10.1039/D3CS00445G
Discovery of a selective TC-PTP degrader for cancer immunotherapy
Jinmin Miao, Jiajun Dong, Yiming Miao, Yunpeng Bai, Zihan Qu, Brenson A. Jassim, Bo Huang, Quyen Nguyen, Yuan Ma, Allison A. Murray, Jinyue Li
DOI: 10.1039/D3SC04541B
Visible light-mediated halogenation of organic compounds
Alexey A. Festa, Olga A. Storozhenko, Leonid G. Voskressensky
DOI: 10.1039/D3CS00366C
Reticular framework materials for photocatalytic organic reactions
Ning-Yu Huang, Yu-Tao Zheng, Di Chen, Zhen-Yu Chen, Chao-Zhu Huang, Qiang Xu
DOI: 10.1039/D2CS00289B
Towards multimodal cellular imaging: optical and X-ray fluorescence
Marcus E. Graziotto, Clinton J. Kidman, Simon A. James, Hugh H. Harris
DOI: 10.1039/D3CS00509G
Unveiling practical considerations for reliable and standardized SERS measurements: lessons from a comprehensive review of oblique angle deposition-fabricated silver nanorod array substrates
Yiping Zhao, Amit Kumar, Yanjun Yang
DOI: 10.1039/D3CS00540B
High-entropy alloys in electrocatalysis: from fundamentals to applications
Jin-Tao Ren, Lei Chen, Hao-Yu Wang
DOI: 10.1039/D3CS00557G
You might also like
What is Ethyl 3-cyclohexylpropanoate (CAS: 10094-36-7)?
Ethyl 3-cyclohexylpropanoate is a clear, colorless to light yellow liquid with a...
How should waste containing 2-(Hydroxymethyl)-5-(methoxycarbonyl)-6-methyl-4-(2-nitrophenyl)nicotinic acid (CAS: 34783-31-8) be handled?
Waste containing 2-(Hydroxymethyl)-5-(methoxycarbonyl)-6-methyl-4-(2-nitrophenyl...
How should waste containing 2,4,6-Tris(pentafluoroethyl)-1,3,5-triazine (CAS: 858-46-8) be handled?
Waste containing 2,4,6-Tris(pentafluoroethyl)-1,3,5-triazine (CAS: 858-46-8) sho...
What precautions should be taken when handling Chloroac-nle-oh (CAS: 56787-36-1)?
When handling Chloroac-nle-oh (CAS: 56787-36-1), it is essential to wear appropr...
What industries use Ethyl 6-phenylimidazo[2,1-b][1,3]thiazole-3-carboxylate (CAS: 752244-05-6)?
Ethyl 6-phenylimidazo[2,1-b][1,3]thiazole-3-carboxylate is primarily used in the...
Are there alternatives to alpha-(2-Bromophenyl)benzylamine (CAS: 55095-15-3) in synthesis?
Alternatives to alpha-(2-Bromophenyl)benzylamine (CAS: 55095-15-3) in synthesis ...
How should waste containing 2-Chloro-5-methoxypyridine (CAS: 139585-48-1) be handled?
Waste containing 2-Chloro-5-methoxypyridine (CAS: 139585-48-1) should be managed...
What industries use 1-(4-Methoxyphenyl)-2,5-dimethyl-1H-pyrrole (CAS: 5044-27-9)?
1-(4-Methoxyphenyl)-2,5-dimethyl-1H-pyrrole (CAS: 5044-27-9) is used in various ...
Are there alternatives to 3-Bromo-5-(N-Boc)aminomethylisoxazole (CAS: 903131-45-3) in synthesis?
There are alternative reagents and compounds that can be used in the synthesis o...
What is Tungsten(IV) oxide (CAS: 12036-22-5)?
Tungsten(IV) oxide, also known as tungsten dioxide, is a chemical compound with ...
Source Journal
Reaction Chemistry & Engineering

Reaction Chemistry & Engineering is an interdisciplinary journal reporting cutting-edge research focused on enhancing the understanding and efficiency of reactions. Reaction engineering leverages the interface where fundamental molecular chemistry meets chemical engineering and technology. Challenges in chemistry can be overcome by the application of new technologies, while engineers may find improved solutions for process development from the latest developments in reaction chemistry. Reaction Chemistry & Engineering is a unique forum for researchers whose interests span the broad areas of chemical engineering and chemical sciences to come together in solving problems of importance to wider society. All papers should be written to be approachable by readers across the engineering and chemical sciences. Papers that consider multiple scales, from the laboratory up to and including plant scale, are particularly encouraged.










![Bis[(1,2,3,4,5-eta)-1-(diphenylphosphino)cyclopentadienyl]iron structure Bis[(1,2,3,4,5-eta)-1-(diphenylphosphino)cyclopentadienyl]iron structure](https://static.chemtradehub.com/structs/121/12150-46-8-ecd2.webp)

![2-{3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl}[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one hydrochloride (1:1) structure 2-{3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl}[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one hydrochloride (1:1) structure](https://static.chemtradehub.com/structs/253/25332-39-2-496e.webp)

