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A kind of preparation method of rabeprazole impurity

A technology for rabeprazole and impurities, which is applied in the field of drug synthesis and achieves the effects of easy availability of raw materials, simple operation method and reasonable process design

Active Publication Date: 2019-05-10
TLC NANJING PHARMA RANDD CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on rabeprazole impurities has not been reported

Method used

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  • A kind of preparation method of rabeprazole impurity
  • A kind of preparation method of rabeprazole impurity
  • A kind of preparation method of rabeprazole impurity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] (1) Dissolve benzyl alcohol in 10-30 volumes of dimethyl sulfoxide, add sodium hydrogen under ice bath, stir for 10 minutes under ice bath, add 2,3-dimethyl-4-chloropyridine-N -oxide, stirred at 30°C-120°C to obtain compound II, the ratio of the amount of substance of compound I, benzyl alcohol and sodium hydrogen, and the screening experimental data of the reaction solvent are as follows:

[0029]

[0030] The experimental data of reaction temperature variation are as follows:

[0031]

[0032] (2) Dissolve 0.31 mol of compound II in 360 mL of acetic acid, add 360 mL of acetic anhydride, heat and stir, and the reaction solution changes from a light red solution to a dark red solution. The reaction solution was cooled to room temperature, concentrated and evaporated to dryness to obtain red solid compound III, the experimental data of reaction temperature and reaction time changes are as follows:

[0033]

[0034] (3) Dissolve compound III in 595 mL of ethanol...

Embodiment 2

[0050] (1) Dissolve benzyl alcohol in 10-30 volumes of dimethylformamide, add sodium hydrogen under ice bath, stir for 10 minutes under ice bath, add 2,3-dimethyl-4-chloropyridine-N -oxide, stirred at 30°C-120°C to obtain compound II, the ratio of the amount of substance of compound I, benzyl alcohol and sodium hydrogen, and the screening experimental data of the reaction solvent are as follows:

[0051]

[0052] The experimental data of reaction temperature variation are as follows:

[0053]

[0054] (2) Dissolve 0.31 mol of compound II in 360 mL of acetic acid, add 360 mL of acetic anhydride, heat and stir, and the reaction solution changes from a light red solution to a dark red solution. The reaction solution was cooled to room temperature, concentrated and evaporated to dryness to obtain red solid compound III, the experimental data of reaction temperature and reaction time changes are as follows:

[0055]

[0056] (3) Dissolve compound III in 595 mL of ethanol,...

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Abstract

The invention discloses a synthesizing method of a rabeprazole sodium impurity, and belongs to the field of medicine synthesis. A preparation method has the advantages that the technology design is reasonable, the operability is strong, the reaction conditions are more moderate, the yield rate is high, and the industrialization production is realized. The preparation method is characterized in that 2,3-dimethyl-4-chloropyridine-N-oxide and 2-chlorobenzimidazole are used as raw materials, and the eight-step reaction is performed, so as to realize the synthesis of the rabeprazole sodium impurity. The prepared rabeprazole sodium impurity has the advantages that the important basis is provided for the scientific evaluation on quality, safety and efficiency of rabeprazole sodium; the pharmacological activity of the rabeprazole sodium impurity is good; the medicines for treating active duodenal ulcer, benign gastric ulcer and duodenal ulcer with positive helicobacter pylori due to various reasons can be developed, and the important application value is realized.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a method for preparing rabeprazole impurities. Background technique [0002] Proton pump inhibitors are the latest generation of acid-suppressing drugs currently in clinical use, with strong and long-lasting acid-suppressing effects. The proton pump acts on the last link in the process of gastric acid secretion. After being absorbed into the blood in the body, it reaches the secretory tubule of the gastric parietal cell, and is transformed into an active substance in an acidic environment, acting on H + -K + -ATPase and inactivation, resulting in the inability of hydrogen ions in the parietal cells to be transferred to the gastric cavity, reducing gastric acid secretion, and increasing the pH value of the gastric juice, thereby achieving acid suppression. [0003] Rabeprazole, omeprazole, lansoprazole, and pantoprazole are a new type of benzimidazole proton pump inhibitor commonly...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/12A61P1/04
CPCC07D401/12
Inventor 何旭胡永铸张池刘春崔希林
Owner TLC NANJING PHARMA RANDD CO LTD
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