A kind of quaternary ammonium salt catalysis and application

Abstract

The invention provides novel 4H-1,2,4-triazole quaternary ammonium salt derivatives (shown as formula I), a preparing method thereof and applications of the derivatives especially as bromination catalysts, and belongs to the technical field of chemical medicine synthesis. Through adding the catalysts to reactions, the reaction activity is increased, reaction temperatures are reduced, the using amounts of bromination agents are greatly reduced, a column chromatography purification step is avoided, and the production cost is reduced. The derivatives are stable and controllable in quality, are suitable for commercial production of medicine intermediates, and make catalysis bromination more environmentally friendly.

Description

technical field

[0001] The invention relates to the field of medicine, and relates to a Lesinurad intermediate 2-(5-bromo-4-(4-cyclopropylnaphthalene-1-yl)- 4H -1,2,4-triazole-3-mercapto) acetate compound quaternary ammonium salt catalyzed preparation method. Background technique

[0002] Gout is a crystal-associated arthropathy caused by the deposition of monosodium urate, which is directly related to hyperuricemia caused by disturbance of purine metabolism or decreased uric acid excretion. Lesinurad is an oral uricosuric agent that inhibits the renal proximal tubule uric acid transporter URAT1. Developed by the British pharmaceutical giant AstraZeneca, it was launched in the United States on December 22, 2015. There are more than 20 million gout patients in the world, so it has a good market prospect.

[0003] Patent CN103524440B has protected Lesinurad brominated intermediate (chemical name is 2-(5-bromo-4-(4-cyclopropylnaphthalene-1-yl)- 4H -1,2,4-triazole-3-mercapto...

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