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Preparation method of bepotastine besilate

A bepotastine benzenesulfonate and electromagnetic control technology are applied in the field of preparation of bepotastine benzenesulfonate, and can solve the problems of difficulty in adding various organic solutions, inconvenience in adding organic solutions, difficult methods for purity, and the like, Achieve the effect of easy recording and quantitative feeding, convenient feeding and saving of extraction steps

Inactive Publication Date: 2021-07-27
浙江天顺药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in the existing related literature, there are very few reports about improving the purity of bepotastine besilate, and the recrystallization method is often used to purify. Although the recrystallization method can obtain bepotastine bepotastine besilate with a purity of 95%, further steps are needed Purify bepotastine bepotastine besilate with a purity of more than 99%, and control the optical isomers below the detection limit. The existing methods for improving the purity are very difficult; some companies have developed methods to remove crude bepotastine besilate However, there are still many problems, such as inconvenient addition of organic solutions, easy leakage during addition, and difficulty in adding various organic solutions, which affect the purification work and low work efficiency. Inconvenient to use

Method used

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  • Preparation method of bepotastine besilate
  • Preparation method of bepotastine besilate
  • Preparation method of bepotastine besilate

Examples

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Embodiment 1

[0036] The invention discloses a preparation method of bepotastine besylate, in a specific embodiment of the invention, comprising the following steps:

[0037] S1: Put the aqueous solution of inorganic alkali into the first reaction chamber of the first reaction kettle, then add the crude product of bepotastine besylate, start the first agitator to stir, and make the crude product of bepotastine besylate Fully mixed and dispersed with inorganic alkali aqueous solution;

[0038] S2: Then open the one-way valve on the first discharge pipe to filter the liquid and flow into the bottom of the partition, then start the first electromagnetic control mechanism to energize the electromagnetic coil, the iron core generates magnetic force, and the piston is sucked downward by the iron core close, drive the piston sleeve to move downward, and open the first valve seat. At this time, both the upper and lower ends of the piston sleeve are opened, the first liquid inlet and the second liqu...

Embodiment 2

[0043] Such as Figure 1 to Figure 5 As shown, the steps in Example 1 are carried out in the first reactor 1, the second reactor 2 and the hollow drying box, wherein, the upper end of the first reactor 1 is provided with a feed port, and the first reactor 1 is provided with a feed inlet. The agitator 3 is arranged in the first reaction kettle 1, and a partition 11 is horizontally installed in the first reaction kettle 1, the first discharge pipe is installed at the lower end of the partition 11, and the one-way valve 13 is installed at the second On a discharge pipe 12, a filter element 14 is installed in the first discharge pipe 12; a connecting pipe 15 is installed on the first reaction kettle 1, and the connecting pipe 15 is located at the lower end of the dividing plate 11, and the connecting pipe 15 is provided with a liquid addition valve 5 for adding organic solution, and a liquid separator 16 is installed on the upper end of the second reaction kettle 2, and a scale is...

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Abstract

The invention provides a preparation method of bepotastine besilate. According to a technical scheme in the invention, the preparation method of bepotastine besilate is characterized by comprising the following step: S1, putting an aqueous inorganic alkali solution into a first reaction cavity of a first reaction kettle, then adding a crude bepotastine besilate product and starting a first stirrer for stirring so as to fully mix and disperse the crude bepotastine besilate product and the aqueous inorganic alkali solution. The preparation method has the beneficial effects that bepotastine besylate is convenient and rapid to prepare and high in stability.

Description

technical field [0001] The invention relates to the technical field of organic chemistry, in particular to a preparation method of bepotastine besylate. Background technique [0002] Bepotastine, chemical name (+)-4-[[(S)-p-chloro-α-2-pyridylbenzyl]oxy]-1-piperidine butanoic acid, English name Bepotastine, clinical Bepotastine Bepotastine is marketed with bepotastine besylate as the active ingredient. Bepotastine besylate is the besylate salt of bepotastine, a drug with antihistamine activity that can be used to treat Allergic diseases such as rhinitis, and skin diseases such as eczema, dermatitis, prurigo, itchy skin, and urticaria. [0003] Existing studies have shown that different isomers of bepotastine besylate have significant differences in pharmacological effects, among which the S isomer has more than 100 times stronger pharmacological effects than the R isomer, and the S isomer binds to plasma proteins The rate is higher than that of the R type, so the less the c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 张胜
Owner 浙江天顺药业有限公司
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