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A kind of preparation method of epinastine hydrochloride

A technology of epilastine hydrochloride and hydrochloric acid method is applied in the field of preparation of epilastine hydrochloride, which can solve the problems of increasing unsafe factors, environmental impact, and inability to ensure that cyanogen bromide will not remain, and achieves reduction of toxicity and improved efficiency. The effect of safety and operation safety

Active Publication Date: 2015-09-16
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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  • A kind of preparation method of epinastine hydrochloride
  • A kind of preparation method of epinastine hydrochloride
  • A kind of preparation method of epinastine hydrochloride

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[0056] The present invention provides a preparation method of epinastine hydrochloride, and those skilled in the art can learn from the content of this article and appropriately improve the process parameters. 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 deemed to be included in the present invention. The method and application of the present invention have been described through the preferred embodiments. It is obvious that relevant persons can modify or appropriately change and combine the methods and applications described herein without departing from the content, spirit and scope of the present invention to achieve and Apply the technology of the present invention.

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

[0058] Step 1: In an organic solvent, a compound having a structure represented by for...

Embodiment 1

[0115] Example 1 Preparation of a compound having the structure shown in Formula III

[0116] According to the raw materials and proportions provided in Table 1, a compound with the structure shown in Formula III was prepared:

[0117] Table 1 Raw materials and proportions required for preparing compounds with the structure shown in formula III

[0118] raw material name

Molecular weight

Dosage

Molar weight

The molar ratio of

S-methyl isothiourea 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, add 5.56 g of S-methyl isothiourea sulfate and 15 mL of dichloromethane to a three-necked flask, stir to dissolve, add 15 mL of saturated sodium bicarbonate solution and 17.44 g of...

Embodiment 2

[0122] Example 2 Preparation of a compound having the structure shown in formula III

[0123] According to the raw materials and proportions provided in Table 2, a compound with the structure shown in Formula III was prepared:

[0124] Table 2 Raw materials and proportions required for preparing compounds with the structure shown in Formula III

[0125] raw material name

Molecular weight

Dosage

Molar weight

The molar ratio of

S-methyl isothiourea 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, add 5.56 g of S-methyl isothiourea sulfate and 15 mL of dichloromethane to a three-necked flask, stir to dissolve, add 15 mL of saturated sodium bicarbonate solution and 8.73 g of d...

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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 medicine, 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 intensification of environmental pollution, the occurrence of allergic diseases has been increasing year by year. Moreover, allergic reactions are involved in the occurrence and development of many diseases, making anti-allergic drugs one of the most commonly used drug classes worldwide. [0003] The English name of Epinastine hydrochloride is epinastine hydrochloride, and the chemical name is 3-amino-9,13-dihydro-1H-dibenzo[c,f]-imidazo[1,5-a]azahydrochloride , Its structure is shown in formula I. It is an oral effecti...

Claims

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Application Information

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