Method for synthesizing 2-(3-cyano-4- isobutoxy phenyl)-4-methyl-carboxylate

Abstract

The invention belongs to the technical field of medicine, and relates to a method for synthesizing 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazole formic acid. The method comprises that: 4-hydroxyl cyanobenzene is used as a raw material, and subjected to iodination, hydrocarbylation and cyanation to obtain an intermediate of 4-isobutoxy-1,3-benzene dinitrile, the intermediate reacts with sodium bisulfide and anhydrous magnesium chloride to obtain a key intermediate of 3-cyano-4-isobutoxy phenyl thioformamide, and the 3-cyano group-4-isobutoxy phenyl thioformamide is subjected to cyclization and hydrolysis reaction to obtain the 2-(3-cyano-4-isobutoxy phenyl)-4-methyl-5-thiazole formic acid. The method has the advantages of easily obtained materials, simple and convenient operation, high yield, low cost and suitability for industrialized production.

Description

technical field

[0001] The invention belongs to the technical field of medicine, relates to a synthesis method of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid, and also relates to its intermediate 4-isobutyl Synthetic method of oxy-1,3-phthalonitrile and 3-cyano-4-isobutoxybenzenethiocarboxamide. Background technique

[0002] Gout is a group of heterogeneous metabolic diseases caused by long-term purine metabolic disorders and / or decreased uric acid excretion. Gout is the second most common metabolic disease in humans after diabetes. The clinical features of gout are hyperuricemia, recurrent acute arthritis, tophi deposition, tophi chronic arthritis and joint deformities, chronic interstitial nephritis and nephrolithiasis caused by kidney involvement. Often complicated by cardiovascular and cerebrovascular diseases and life-threatening. The prerequisite for the onset of gout is hyperuricemia. Hyperuricemia refers to the uric acid content in serum at 37...

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