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Synthesis of domperidone maleate

A technology for domperidone maleate and its synthesis method, which is applied in the directions of pharmaceutical formulations, organic active ingredients, and medical preparations containing active ingredients, etc., and can solve the problems of complex production process, high cost, and low yield of domperidone maleate, Achieve the effect of being convenient for industrialized production, low cost and high yield

Active Publication Date: 2006-08-02
NANJING CHANGAO PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved in the present invention is exactly the problem that present domperidone maleate production process is complicated, yield is low, and cost is higher

Method used

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  • Synthesis of domperidone maleate
  • Synthesis of domperidone maleate
  • Synthesis of domperidone maleate

Examples

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Embodiment Construction

[0045] The following examples are intended to illustrate certain preferred embodiments of the present invention and are not intended to limit the scope of the present invention.

[0046] 1, Synthesis of 2(3H) benzimidazolone (I)

[0047] Add 448g of o-diaminobenzene and 1000ml of toluene into a 2.5L reaction flask, raise the temperature to 60-70°C, within 6 hours, slowly add 496g of ethyl chloroformate and 502g of triethylamine dropwise at the same time, and control the pH value at Between 8 and 11, keep the reaction for 6 hours under the condition of 60-70°C after dropping. After cooling to 5~-10°C, a solid was precipitated, filtered, washed with water, and dried to obtain 513g of product with a melting point of >300°C and a yield of 92.1%.

[0048] 2. Synthesis of 1-(3-chloropropyl)-1,3-dihydro-2H-benzimidazol-2-one (II)

[0049] Add 446g of I, 577g of 1-bromo-3-chloropropane and 1340ml of 10% sodium hydroxide solution in the reaction flask, stir and dissolve at room tempe...

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Abstract

The present invention relates to synthesis process of 5-chloro-1-[1-[3-(2, 3-dihydro-2-oxo-1H-benzimidazol-1-yl)-propyl]-4-piperidyl]-1, 3-dihydro-2H-benzimidazol -2-one(Z)-butene diacid, i. e., domperidone maleate. O-diaminobenzene is first cyclized and halogenated to form the first benzimidazolone intermediate; 1-carbethoxy-4-amino piperidine is halogenated, reduced, cyclized and hydrolyzed to form the second benzimidazolone intermediate; the two benzimidazolone intermediates are reacted to produce domperidone; and domperidone is finally reacted with maleic aicd to produce domperidone maleate. The process of the present invention has short reaction period, high yield, low cost and other advantages is suitable for industrial production.

Description

technical field [0001] The present invention relates to a kind of 5-chloro-1-[1-[3-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-propyl]-4-piperidinyl] -1,3-Dihydro-2H-benzimidazol-2-one (Z)-butenedioic acid, namely domperidone maleate, is a synthetic method. Background technique [0002] Domperidone maleate is a peripheral dopamine receptor blocker that acts directly on the gastrointestinal wall to increase the tension of the lower esophageal sphincter, prevent gastroesophageal reflux, enhance gastric motility, promote gastric emptying, and coordinate the stomach and duodenum Exercise can inhibit nausea and vomiting, and can effectively prevent bile reflux without affecting gastric juice secretion. Domperidone does not easily pass through the blood-cerebrospinal fluid barrier and has no inhibitory effect on dopamine receptors in the brain. Therefore, it has no extrapyramidal and other neurological and mental adverse reactions. Domperidone is rapidly absorbed after oral adminis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14A61K31/454
Inventor 李战刘彩连李纬曹芳
Owner NANJING CHANGAO PHARM CO LTD
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