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Preparation method of pyrimidine derivative

A technology of pyrimidine derivatives and methylpyrimidine, which is applied in the field of preparation of pyrimidine derivatives 2-methoxy-5-benzoic acid, and can solve problems such as difficult synthesis

Inactive Publication Date: 2015-07-29
长沙深橙生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The synthesis of 2-methoxy-5-(2-methylpyrimidin-4-yl)benzoic acid is difficult at present

Method used

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  • Preparation method of pyrimidine derivative
  • Preparation method of pyrimidine derivative
  • Preparation method of pyrimidine derivative

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0024] (1) Synthesis of 5-acetyl-2-hydroxybenzoic acid isopropyl ester

[0025] Add 20g of isopropyl salicylate to 250ml of dichloromethane, add 31g of anhydrous aluminum trichloride and 29g of acetyl chloride, stir at room temperature for 3 hours, add ice water and ethyl acetate, extract and separate, collect the organic phase, Drying and concentration gave 23 g of isopropyl 5-acetyl-2-hydroxybenzoate.

[0026] (2) Synthesis of 5-acetyl-2-methoxyisopropyl benzoate

[0027] Add 22g of isopropyl 5-acetyl-2-hydroxybenzoate to 160ml of N,N-dimethylformamide, add 25g of anhydrous potassium carbonate, then add 27g of methyl iodide, heat to 50°C, and stir at reflux for 2 Hours, cooling, adding water and ethyl acetate for extraction and separation, collecting the organic phase, washing with water three times, drying the organic phase, concentrating, and column separation to obtain 19g of isopropyl 5-acetyl-2-methoxybenzoate.

[0028] (3) Synthesis of (E)-isopropyl-5-(3-(dimethylami...

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Abstract

The invention discloses a preparation method of a pyrimidine derivative 2-methoxy-5-(2-methylpyrimidine-4-yl)benzoic acid. Isopropyl salicylate is taken as a starting material, and a target product is obtained through acetylation, methylation, acryl acylation, ring closing and hydrolysis reactions. A variety of compound libraries are synthesized with the products serving as template micro-molecules.

Description

technical field [0001] The invention relates to a preparation method of a pharmaceutical intermediate, in particular to a preparation method of a pyrimidine derivative 2-methoxy-5-(2-methylpyrimidin-4-yl)benzoic acid. technical background [0002] Compound 2-methoxy-5-(2-methylpyrimidin-4-yl)benzoic acid, the structural formula is: [0003] [0004] The compound 2-methoxy-5-(2-methylpyrimidin-4-yl)benzoic acid and related derivatives are widely used in medicinal chemistry and organic synthesis. Currently, the synthesis of 2-methoxy-5-(2-methylpyrimidin-4-yl)benzoic acid is difficult. Therefore, it is necessary to develop a synthetic method with easy-to-obtain raw materials, convenient operation, easy-to-control reaction and suitable overall yield. Contents of the invention [0005] The invention discloses a preparation method of a pyrimidine derivative 2-methoxy-5-(2-methylpyrimidin-4-yl)benzoic acid, which uses isopropyl salicylate as a starting material, undergoes a...

Claims

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Application Information

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IPC IPC(8): C07D239/26
CPCC07D239/26
Inventor 不公告发明人
Owner 长沙深橙生物科技有限公司