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Preparation method of epinastine hydrochloride

A technology of epinastine hydrochloride and hydrochloric acid method, which is applied in the field of preparation of epinastine hydrochloride, can solve the problems of increasing unsafe factors, the inability to ensure that cyanogen bromide will not remain, and environmental impact, so as to reduce toxicity and improve Effects on safety and operational safety

Active Publication Date: 2013-06-26
BEIJING JINCHENG TAIER PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, adopt above-mentioned method to synthesize epinastine hydrochloride not only need to prevent that cyanogen bromide leaks and cause injury to the operator in the preparation process, and can't guarantee that cyanogen bromide can not remain in the epinastine hydrochloride that makes, increase The unsafe factors of medication are eliminated, and a large amount of toxic substances are used for preparation, which will also have an impact on the environment

Method used

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  • Preparation method of epinastine hydrochloride
  • Preparation method of epinastine hydrochloride
  • Preparation method of epinastine hydrochloride

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preparation example Construction

[0056] The invention provides a method for preparing epinastine hydrochloride, which can be realized by appropriately improving process parameters for reference by those skilled in the art. In particular, it should be pointed out that all similar replacements and modifications are obvious to those skilled in the art, and they are all considered to be included in the present invention. The method and application of the present invention have been described through preferred embodiments, and the relevant personnel can obviously make changes or appropriate changes and combinations to the method and application described herein without departing from the content, spirit and scope of the present invention to realize and Apply the technology of the present invention.

[0057] The invention provides a kind of preparation method of epinastine hydrochloride, comprises the following steps:

[0058] Step 1: In an organic solvent, the compound having the structure shown in formula II is ...

Embodiment 1

[0115] Embodiment 1 has the preparation of structure compound shown in formula III

[0116] According to the raw materials and proportioning that table 1 provides, prepare the compound with the structure shown in formula III:

[0117] The preparation of table 1 has the required raw materials and proportioning of structural compounds shown in formula III

[0118] raw material name

molecular weight

Dosage

molar weight

The molar ratio of

S-methylisothiourea sulfate

278.38

5.56g

0.02

1

Di-tert-butyl dicarbonate

218.25

17.44g

0.08

4

Dichloromethane

84.93

75mL

1.17

Saturated sodium bicarbonate solution

84.01

15mL

saturated sodium chloride solution

58.44

20mL

purified water

18.02

15mL

Anhydrous Magnesium Sulfate

120.36

5g

[0119] The preparation method is as follows: First...

Embodiment 2

[0122] Embodiment 2 has the preparation of structure compound shown in formula III

[0123] According to the raw materials and proportioning that table 2 provides, prepare the compound with the structure shown in formula III:

[0124] The preparation of table 2 has the required raw materials and proportioning of structural compounds shown in formula III

[0125] raw material name

molecular weight

Dosage

molar weight

The molar ratio of

S-methylisothiourea sulfate

278.38

5.56g

0.02

1

Di-tert-butyl dicarbonate

218.25

8.73g

0.04

2

Dichloromethane

84.93

75mL

1.17

Saturated sodium bicarbonate solution

84.01

15mL

saturated sodium chloride solution

58.44

20mL

purified water

18.02

15mL

Anhydrous Magnesium Sulfate

120.36

5g

[0126]The preparation method is as follows: First, ...

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Abstract

The invention relates to the technical field of medicine, in particular to a preparation method of epinastine hydrochloride. The preparation method comprises the following steps: performing substitution reaction of a compound with a structure as shown in formula (II) and a compound with a structure as shown in formula (III) in an organic solvent, so as to produce a compound with a structure as shown in formula (IV); cyclizing the compound with the structure as shown in formula (IV) in the organic solvent in the presence of p-toluene sulphonic acid, so as to produce a compound with a structure as shown in formula (V); and then salifying the compound with the structure as shown in formula (V), so as to produce a compound with the structure as shown in formula (I). Thus, cyanogens bromide which is used in the traditional preparation method is prevented from being used in the cyclizing reaction, and therefore the toxicity of the preparation method is reduced. The operation of the preparation method is safer and more environment-friendly.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a preparation method of epinastine hydrochloride. Background technique [0002] Allergic diseases are common clinical diseases, including allergic bronchial asthma, allergic rhinitis, allergic skin diseases and urticaria. For a long time, allergic diseases have been threatening human health, especially in recent decades with the progress of industrialization and the aggravation of environmental pollution, the incidence of allergic diseases has been increasing year by year. Moreover, allergic reactions are involved in the occurrence and development of many diseases, making antiallergic drugs one of the most commonly used drug categories in the world. [0003] Epinastine hydrochloride is called epinastine hydrochloride in English, and its chemical name is 3-amino-9,13-dihydro-1H-dibenzo[c,f]-imidazo[1,5-a]azepine hydrochloride , whose structure is shown in formula I. It is an ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
Inventor 杨军
Owner BEIJING JINCHENG TAIER PHARMA CO LTD
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