Preparation method of roxatidine acetate hydrochloride

A technology of roxatidine hydrochloride acetate and ethyl acetate, which is applied in the field of preparation of roxatidine hydrochloride acetate, and can solve the problems of intense reaction process, excessive product impurities, and difficult control of reaction conditions, etc.

Active Publication Date: 2017-06-23
HAYAO GRP SANJING MINGSHUI PHARMA CO LTD
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  • Abstract
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  • Application Information

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Problems solved by technology

At present, roxatidine hydrochloride acetate is mostly synthesized by chemical methods in the world. In the synthetic method, there are many shortcomings such as intense reaction process, uneasy control of reaction conditions, low yield, long production cycle, high production cost, and excessive impurities in the product.

Method used

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  • Preparation method of roxatidine acetate hydrochloride
  • Preparation method of roxatidine acetate hydrochloride
  • Preparation method of roxatidine acetate hydrochloride

Examples

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Embodiment Construction

[0024] Specific embodiments of the invention

[0025] Take 1246g of m-hydroxybenzaldehyde, put it in a microwave reactor, add 2600g of hexahydropyridine, cool, add 400g of sodium borohydride, 5000g of absolute ethanol, 20g of aluminum chloride, select a microwave frequency of 2400MHz, react for 2 hours, and distill under reduced pressure , to obtain a solid, add 0.1M hydrochloric acid to dissolve, add ethyl acetate 4000g to extract, adjust the pH value of the aqueous phase to 9 with 25% ammonia water, add petroleum ether 2000g, stir for 1 hour, and precipitate a white solid;

[0026] Take 1500g of the above-mentioned white solid, put it in a microwave reactor, add 540g of 70% sodium hydride and 3000g of anhydrous dimethylformamide, select a microwave frequency of 1500MHz, react for 1 hour, add 500g of sodium hydroxide, 400g of potassium hydroxide, and then Add 1330g of 3-chloropropylamine hydrochloride and 4000g of anhydrous dimethylformamide, select a microwave frequency of 2...

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Abstract

The invention discloses a preparation method of roxatidine acetate hydrochloride. The preparation method is characterized by adopting m-hydroxybenzaldehyde and piperidine as raw materials for carrying out chemical synthesis under the conditions of microwave radiation and high frequency ultrasonic wave, so that the product yield is improved, the reaction time is shortened, the cost is reduced, the product purity is improved, the total impurities are reduced, and an ideal effect is achieved.

Description

technical field [0001] The invention relates to the field of chemical medicine preparation, in particular to a preparation method of roxatidine hydrochloride acetate. Background technique [0002] Roxatidine hydrochloride acetate is a histamine H2 receptor antagonist, long-acting, well tolerated, has no anti-androgen effect, and does not hinder drug metabolism in the liver. It can be used for gastric ulcer, duodenal ulcer, anastomotic ulcer, Zoller-Ellison syndrome, reflux esophagitis, etc. At present, roxatidine hydrochloride acetate is mostly synthesized by chemical methods in the world. In the synthetic method, there are severe reaction process, difficult control of reaction conditions, low yield, long production cycle, high production cost, and excessive product impurities. In order to overcome the above-mentioned shortcomings, the present invention explores the synthesis process of roxatidine hydrochloride acetate, adopts microwave radiation synthesis technology, high-...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): C07D295/096
CPCC07D295/096
Inventor秦洪波林长松赵业辉魏岩庞树和
OwnerHAYAO GRP SANJING MINGSHUI PHARMA CO LTD