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Synthesis method of ranitidine alkali and its hydrochloride

A technology of ranitidine base and synthesis method, which is applied in the synthesis field of ranitidine base and its hydrochloride, can solve the problems of residue, influence, increased cost and the like, and achieves low cost, simple process and easy industrial production. Effect

Active Publication Date: 2006-01-25
石药集团中诺药业(石家庄)有限公司
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  • Application Information

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Problems solved by technology

In the method disclosed in the prior art, multiple organic solvents are used, such as chloroform, isopropanol and n-hexane, etc., which not only increase the cost in production, but also the solvent used remains in the ranitidine base, which will be used in the preparation of radine hydrochloride. effects of nitidine

Method used

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  • Synthesis method of ranitidine alkali and its hydrochloride
  • Synthesis method of ranitidine alkali and its hydrochloride

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Embodiment Construction

[0016] 1. Add 367.5kg of 2-[[[5-(dimethylamino)methyl-2-furyl]methyl]thio]ethylamine and 655kg of purified water into the reaction tank, and add 1-methylthio under stirring - 245kg of 1-methylamino-2-nitroethylene, the molar ratio of the two reactants is 1.04:1, the temperature is slowly raised to 48-52°C, the vacuum degree is controlled at 0.02-0.05Mpa, and the reaction is kept for 4.5 hours, and the reaction is completed.

[0017] Use cold brine to cool the feed liquid to about 25°C-35°C, adjust the base with 10% sodium hydroxide solution, and measure it with a pH meter until pH = 11.00-11.40. Crystallize at ~2°C, freeze for 12 hours and filter, rinse the filter cake with 50-70kg of purified water per centrifuge to obtain the wet product of ranitidine base. The reaction equation is as follows

[0018]

[0019] 2. Put the wet ranitidine base into the concentration tank, the temperature in the tank is below 65°C, and the vacuum degree is 0.09-0.098Mpa, distill water, after...

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Abstract

The invention provides a method for synthesis of ranitidine alkali and ranitidine hydrochloride. It is characterized in that: 2- [ [ [5- (dimethylamino) methyl- 2- furyl] methyl] sulpho] ethylamine reacts with 1- methylthio - 1- methylamino- 2- nitro ethylene directly in water phase, crystallizing and separating out ranitidine alkali. The synthesis method comprises the following steps: adding 2- [ [ [5- (dimethylamino) methyl- 2- furyl] methyl] sulpho] ethylamine and 1- methylthio- 1- methylamino- 2- nitro ethylene with a molar ratio of 1.04: 1 into water, heating to 48- 52 Deg. C, reacting 4.5 hours with a vacuum degree of 0.02- 0.05 MPa, cooling, adding sodium-hydroxide of concentration of 10% to regulate the PH value to 11.0- 11.4, filtrating and cooling the filtrate to 0- 2 Deg. C, crystallizing for 12 hours, centrifugally filtrating, and rinsing filter cake with purity water to prepare wet ranitidine alkali; dissolving ranitidine alkali in alcohol and reacting with chlorhydric acid to prepare ranitidine hydrochloride.

Description

technical field [0001] The invention relates to a synthesis method of ranitidine base and its hydrochloride, belonging to the technical field of synthesis methods of pharmaceutical and chemical raw materials. Background technique [0002] Ranitidine hydrochloride is a H 2 - Receptor antagonist, which has obvious inhibitory effect on gastric acid secretion caused by physiology and pentagastrin, which is 4-6 times stronger than cimetidine and lasts longer. An ideal drug for ulcers. U.S. Patent No. 5,696,275 discloses a synthetic technique of ranitidine base, which is to combine 2-[[[5-(dimethylamino)methyl-2-furyl]methyl]thio]ethylamine with 1-methyl Sulfuryl-1-methylamino-2-nitroethylene reacted in water, stirred and heated at 45-50°C, reacted for 3-4 hours, then acidified with hydrochloric acid, extracted with chloroform, and then alkalized with potassium carbonate. After adding low-carbon alcohols (isopropanol, etc.) to azeotropically remove water, add n-hexane, cool dow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/52
Inventor 李勇王忠王月辉张士文梁平珍刘光宇
Owner 石药集团中诺药业(石家庄)有限公司
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