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Preparation method of ranitidine hydrochloride

A technology of ranitidine hydrochloride and ranitidine base, which is applied in the field of medicine, can solve the problems of inapplicability to mass production, high processing costs, and cumbersome steps, and achieve the effects of reducing production costs, simple steps, and high purity

Inactive Publication Date: 2018-04-17
孙婷婷
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the existing technology for the preparation of ranitidine has cumbersome steps, low yield and high processing cost, and is not suitable for mass production

Method used

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  • Preparation method of ranitidine hydrochloride
  • Preparation method of ranitidine hydrochloride
  • Preparation method of ranitidine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation method of described ranitidine hydrochloride comprises the following processing steps:

[0026] (1) Add 0.3 mol of 2-chloromethyl-5-dimethylaminofuran and 0.3 mol of cysteamine to basic alumina, reflux and stir for 20 minutes, cool to room temperature, add haloalkane, and reflux for 1 to 2.5 hours , complete S-alkylation to obtain 2-[[[5-[(dimethylamino)methyl]furanmethyl]thio]ethylamine;

[0027] (2) Put 0.1 mol of 2-[[[5-[(dimethylamino)methyl]furanmethyl]thio]ethylamine prepared in step (1) into water, add 0.05 mol of N-methyl-1-methylthio-2-nitroethyleneamine, heated and stirred for 3 to 4 hours, then added hydrochloric acid to make it acidified to obtain a mixed reactant, which was added to chloroform to extract Finally, add potassium carbonate to alkalize, then add isopropanol to azeotropically remove water, then add n-ethane to cool down and crystallize to obtain ranitidine base;

[0028] (3) Use the ranitidine base prepared in step (2) to track...

Embodiment 2

[0037] The preparation method of described ranitidine hydrochloride comprises the following processing steps:

[0038] (1) Add 0.3 mol of 2-chloromethyl-5-dimethylaminofuran and 0.5 mol of cysteamine to basic alumina, reflux and stir for 20 minutes, cool to room temperature, add haloalkane, and reflux for 1 to 2.5 hours. Complete S-alkylation to produce 2-[[[5-[(dimethylamino)methyl]furylmethyl]thio]ethylamine;

[0039] (2) Put 0.1 mol of 2-[[[5-[(dimethylamino)methyl]furanmethyl]thio]ethylamine prepared in step (1) into water, and add 0.1 molN-methyl-1-methylthio-2-nitroethyleneamine, heated and stirred for 3 to 4 hours, then added hydrochloric acid to make it acidified to obtain a mixed reactant, which was added to chloroform, and after extraction, Add potassium carbonate to alkalinize, then add isopropanol to remove water azeotropically, then add n-ethane to cool down and crystallize to obtain ranitidine base;

[0040] (3) Use the ranitidine base prepared in step (2) to t...

Embodiment 3

[0045] The preparation method of described ranitidine hydrochloride comprises the following processing steps:

[0046] (1) Add 0.3 mol of 2-chloromethyl-5-dimethylaminofuran and 0.6 mol of cysteamine to basic alumina, reflux and stir for 20 minutes, cool to room temperature, add halogenated alkanes, and reflux for 1 to 2.5 hours to complete S-alkylation to produce 2-[[[5-[(dimethylamino)methyl]furylmethyl]thio]ethylamine;

[0047] (2) Put 0.1 mol of 2-[[[5-[(dimethylamino)methyl]furanmethyl]thio]ethylamine prepared in step (1) into water, and add 0.2 mol of N-methyl-1-methylthio-2-nitroethyleneamine, heated and stirred for 3 to 4 hours, then added hydrochloric acid to make it acidified to obtain a mixed reactant, which was added to chloroform to extract Finally, add potassium carbonate to alkalize, then add isopropanol to azeotropically remove water, then add n-ethane to cool down and crystallize to obtain ranitidine base;

[0048] (3) Use the ranitidine base prepared in ste...

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Abstract

The invention discloses a preparation method of ranitidine hydrochloride, the chemical name of said ranitidine hydrochloride is N'-methyl-N-[2[[5-[(dimethylamino)methyl-2-furan Base] methyl] thio] ethyl]-2-nitro-1,1-ethylenediamine hydrochloride, the chemical structural formula of said ranitidine hydrochloride is, and the molecular formula of said ranitidine hydrochloride is C13H22N4O3S ·HCl: the invention has simple steps, higher yield than the existing level, high purity, reduced production cost, and is suitable for mass production.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of ranitidine hydrochloride. Background technique [0002] Ranitidine hydrochloride is currently a H2 receptor antagonist with wide clinical application and good curative effect. It is mainly used for the treatment of duodenal ulcer, benign gastric ulcer, postoperative ulcer, reflux esophagitis and so on. [0003] Ranitidine is the main raw material for the preparation of ranitidine hydrochloride, ranitidine hydrochloride, English name: RanitidineLeinitiding Piam, its pharmacology has the effect of competitively blocking the combination of histamine and H2 receptors, and inhibits the action of gastric acid. It is calculated as 5 to 12 times that of cimetidine, so it is a potent H2 receptor blocker. It is mainly used in the treatment of duodenal ulcer, gastric ulcer, reflux esophagitis, Zollinger-Ellison syndrome and other diseases with high gastric acid sec...

Claims

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Application Information

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IPC IPC(8): C07D307/52
CPCC07D307/52
Inventor 孙婷婷
Owner 孙婷婷
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