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Pantoprazole sodium and preparation method thereof

A technology of pantoprazole sodium and benzimidazole, applied in the field of medicine, can solve problems such as many side reactions, cumbersome steps and the like

Active Publication Date: 2013-08-07
CHENGDU TIANTAISHAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] Chinese patent CN101475561A discloses the preparation method of pantoprazole sodium monohydrate, and this method step is loaded down with trivial details, and side reaction is more

Method used

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  • Pantoprazole sodium and preparation method thereof

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preparation example Construction

[0104] In the steps of the above-mentioned preparation method of the present invention, although the specific steps described in it are different from the steps described in the preparation examples of the specific embodiment section below in some details or language descriptions, those skilled in the art according to The detailed disclosure of the present invention in its entirety can fully summarize the method steps described above.

[0105] Any embodiment of any aspect of the present invention may be combined with other embodiments as long as they do not contradict each other. In addition, in any embodiment of any aspect of the present invention, any technical feature can be applied to the technical feature in other embodiments, as long as there is no contradiction between them.

[0106] The present invention will be further described below.

[0107] All the documents cited in the present invention are incorporated herein by reference in their entirety, and if the meaning ...

specific Embodiment approach

[0110] The present invention can be further described by the following examples, however, the scope of the present invention is not limited to the following examples. Those skilled in the art can understand that various changes and modifications can be made in the present invention without departing from the spirit and scope of the present invention. The present invention provides general and / or specific descriptions of the materials and test methods used in the tests. While many of the materials and methods of manipulation which are employed for the purposes of the invention are well known in the art, the invention has been described here in as much detail as possible. The following examples further illustrate the invention without limiting it.

[0111] test methods:

[0112] The content determination of the main components in various samples (which can be synthetic intermediates, raw materials and preparation intermediates and preparations made from raw materials) can be ...

Embodiment 1

[0151] Embodiment 1: Preparation of 2-chloromethyl-3,4-dimethoxypyridine hydrochloride (III)

[0152]

[0153] Add 9.22kg of toluene, add 1.5kg of 2-hydroxymethyl-3,4-dimethoxypyridine at room temperature, cool down to 3°C-10°C, add 1.63kg of chloride within 1-2 hours at 3-10°C After the addition of sulfoxide, keep stirring at 5-10°C for 1 hour, heat up to 35-40°C within 1 hour, and keep warm at 35-40°C for 4 hours. TLC detection After the reaction is completed, the temperature is controlled at 35-40°C, vacuum distilled thionyl chloride for 3-4 hours, and 9kg of toluene is added, the temperature is lowered to 20-25°C, centrifugal suction filtration, 0.64L toluene washes the filter cake, drains, 50 Blast drying at -55°C for 6-8 hours to obtain 2-chloromethyl-3,4-dimethoxypyridine hydrochloride (III).

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Abstract

The invention relates to pantoprazole sodium and a preparation method thereof and in particular relates to a method for preparing the pantoprazole sodium. The preparation method comprises the following steps of: (1) with 2-hydroxymethyl-3,4-dimethoxyl pyridine (II) as a starting material, generating 2-chloromethyl-3,4-dimethoxyl pyridine hydrochloride (III) under the action of chlorides; (2) carrying out condensation on the obtained compound (III) and 5-difluoromethoxyl-2-sulfydryl-1H-benzimidazole in the presence of inorganic base to generate 5-difluoromethoxyl-2-[(3,4-dimethoxyl-2-pyridyl) methyl] sulfenyl-1H-benzimidazole (IV); (3) oxidizing the obtained compound (IV) by using an oxidant to generate 5-difluoromethoxyl-2-[(3,4-dimethoxyl-2-pyridyl) methyl] sulfinyl-1H-benzimidazole; (4) enabling the 5-difluoromethoxyl-2-[(3,4-dimethoxyl-2-pyridyl) methyl] sulfinyl-1H-benzimidazole to react with sodium hydroxide to generate a salt, namely the pantoprazole sodium (I); and optionally (5) refining the prepared pantoprazole sodium. According to the preparation method, the prepared pantoprazole sodium product has high purity.

Description

technical field [0001] The invention belongs to the technical field of medicines and relates to pantoprazole sodium which can be used for treating stomach diseases. Pantoprazole sodium of the present invention has good properties. Background technique [0002] Digestive system disease is a common and frequently-occurring disease, and it is also a chronic disease that is very easy to relapse. So far, there is no effective way to completely cure it. This has become one of the key topics in the field of pharmaceutical research. Statistical analysis shows that the incidence rate of digestive system diseases in the world accounts for 10-12% of human beings, and the incidence rate of digestive system diseases in cities and towns in my country is 11.43%, which is basically similar to many developed countries in Europe and America. Due to the characteristics of diet structure, the prevalence rate of residents in southern cities and southwestern regions is relatively high, and the i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 赵东明方专王敬江威余帮学董国明
Owner CHENGDU TIANTAISHAN PHARMA
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