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6-(3,4-substituted phenyl)-2-pyrimidinethiol-4-formate compound as well as preparation method and application thereof

A technology for mercaptopyrimidine and compound, which is applied to 6--2-mercaptopyrimidine-4-carboxylic acid compound and its preparation, and the field of medicine for treating gout, achieves the effects of good yield and simple and feasible preparation method

Active Publication Date: 2018-10-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 6-(3,4-substituted phenyl)-2-mercaptopyrimidine-4-carboxylic acid compounds as xanthine oxidase inhibitors have not been reported yet

Method used

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  • 6-(3,4-substituted phenyl)-2-pyrimidinethiol-4-formate compound as well as preparation method and application thereof
  • 6-(3,4-substituted phenyl)-2-pyrimidinethiol-4-formate compound as well as preparation method and application thereof
  • 6-(3,4-substituted phenyl)-2-pyrimidinethiol-4-formate compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1: Preparation of 6-(3-bromo-4-isopropoxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid (Compound 1)

[0073] (Z)-4-(3-bromo-4-isopropoxyphenyl)-2-hydroxy-4-oxobut-2-enoic acid (0.66g, 2mmol), thiourea (0.76g, 10mmol) ), added to glacial acetic acid (30 mL), heated to 100 °C and reacted for 8 hours. After the system was cooled to room temperature, the organic solvent was removed under reduced pressure, and the solid was purified by column chromatography to obtain 6-(3-bromo-4-isopropoxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid.

[0074] The yield of 6-(3-bromo-4-isopropoxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid (compound 1) is 66%, and its structural formula, 1 H-NMR and MS data are listed in Table-1 below.

Embodiment 2

[0075] Example 2: Preparation of 6-(3-bromo-4-isobutoxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid (compound 2)

[0076] 6-(3-Bromo-4-isobutoxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid ( Compound 2), the yield is 71%, its structural formula, 1 H-NMR and MS data are listed in Table-1 below.

Embodiment 3

[0077] Example 3: Preparation of 6-(3-bromo-4-isoamyloxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid (compound 3)

[0078] 6-(3-Bromo-4-isoamyloxyphenyl)-2-mercaptopyrimidine-4-carboxylic acid (Compound 3) was prepared in the same manner as in Example 1, the yield was 67%, and its structural formula, 1 H-NMR and MS data are listed in Table-1 below.

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PUM

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Abstract

The invention belongs to the technical field of medicine, and relates to a 6-(3,4-substituted phenyl)-2-pyrimidinethiol-4-formate compound with xanthine oxidase inhibitory activity shown as a generalformula I, a medicinal salt, a medicinal solvate and a preparation method thereof. The invention further relates to application of these compounds to preparation of medicaments for treating hyperuricemia and gout disease. The general structural formula of the 6-(3,4-substituted phenyl)-2-pyrimidinethiol-4-formate compound is shown in the description, wherein R and X are described in the claims anddescription. The general structural formula is shown in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to 6-(3,4-substituted phenyl)-2-mercaptopyrimidine-4-carboxylic acid compounds and a preparation method and application thereof; in particular, it relates to 6-(3,4-substituted phenyl) -2-Mercaptopyrimidine-4-carboxylic acid compounds, pharmaceutically acceptable salts, pharmaceutically acceptable solvates and preparation methods thereof, and uses of these compounds in the preparation of medicines for treating gout. Background technique [0002] Gout is a series of inflammatory reactions caused by the disturbance of purine metabolism in the body or the reduction of uric acid excretion, which leads to the deposition of uric acid in joints and other places in the body. With the change of people's dietary structure and the increase of intake of animal protein and fat, hyperuricemia and gout patients have a significant increase trend, which has become a global metabolic disease. Gout is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/40A61P19/06
CPCA61P19/06C07D239/40
Inventor 张为革石爱龙王赫张利超王思博杨明正包凯关奇
Owner SHENYANG PHARMA UNIVERSITY
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