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Butanedisulfonic acid dabigatran etexilate and preparation method and application thereof

A technology of dabigatran etexilate and butanedisulfonic acid, applied in the field of medicine, can solve the problems of not clearly providing examples and the like

Active Publication Date: 2014-06-18
海思科制药(眉山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned patent also protects the physiologically acceptable salts of dabigatran etexilate, and mentions that the acids suitable for salifying dabigatran etexilate include hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, fumaric acid, succinic acid, Lactic acid, citric acid, tartaric acid, maleic acid, but no specific examples are provided

Method used

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  • Butanedisulfonic acid dabigatran etexilate and preparation method and application thereof
  • Butanedisulfonic acid dabigatran etexilate and preparation method and application thereof
  • Butanedisulfonic acid dabigatran etexilate and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] The preparation of dabigatran etexilate and crystal form A shown in embodiment 1 formula IV

[0091] Add 2.0 g (3.2 mmol) of dabigatran etexilate into a reaction flask containing 20 ml of acetone, control the temperature at about 30°C, and stir to dissolve it. Dissolve 0.35g (1.6mmol) of 1,4-butanedisulfonic acid in 10ml of acetone, add dropwise to the acetone solution of dabigatran etexilate, continue to stir and crystallize after the dropwise addition, filter, and filter the cake with acetone 10ml was washed and dried under vacuum at 40-45°C to obtain the title product.

[0092] With Bruke AV-II 300MHz nuclear magnetic resonance instrument, deuterated dimethyl sulfoxide is used as test solvent, tetramethylsilane is used as internal standard, and the obtained title product has been carried out at room temperature by proton nuclear magnetic resonance spectrum measurement, the result is:

[0093] 1 H-NMR (300MHz, DMSO-d 6 ,δ / ppm): 11.87(s,1H),10.68(s,1H),10.04(s,1H),8...

Embodiment 2

[0099] The preparation of dabigatran etexilate and its crystal form A shown in embodiment 2 formula IV

[0100] Add 2.0 g (3.2 mmol) of dabigatran etexilate into a reaction flask containing 20 ml of acetone, control the temperature at about 30°C, and stir to dissolve it. Dissolve 0.28g (1.3mmol) of 1,4-butanedisulfonic acid in 5ml of acetone, add dropwise to the acetone solution of dabigatran etexilate, continue to stir and crystallize after the dropwise addition, filter, and use acetone for the filter cake 10ml was washed, and vacuum-dried at 45-50°C to obtain the title product.

Embodiment 3

[0101] The preparation of dabigatran etexilate and its crystal form B shown in embodiment 3 formula V

[0102] Add 3.14g (5.0mmol) of dabigatran etexilate into a reaction bottle containing 30ml of tetrahydrofuran, control the temperature at about 30°C, and stir to dissolve it. Disperse 0.79g (3.6mmol) of 1,4-butanedisulfonic acid in 20ml of tetrahydrofuran, add dropwise to the above-mentioned tetrahydrofuran solution of dabigatran etexilate, continue to stir and crystallize after the dropwise addition, filter, and filter the cake with tetrahydrofuran 10ml was washed and dried under vacuum at 40-45°C to obtain the title product.

[0103] With Bruke AV-II 300MHz nuclear magnetic resonance instrument, deuterated dimethyl sulfoxide is used as test solvent, tetramethylsilane is used as internal standard, and the obtained title product has been carried out at room temperature by proton nuclear magnetic resonance spectrum measurement, the result is:

[0104] 1 H-NMR (300MHz, DMSO-d...

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Abstract

The invention discloses a butanedisulfonic acid dabigatran etexilate and a preparation method thereof, a pharmaceutical composition with butanedisulfonic acid dabigatran etexilate as an active component, and an application of the butanedisulfonic acid dabigatran etexilate and the pharmaceutical composition in preparing drugs for prevention or treatment of diseases caused by thrombus or embolism. The butanedisulfonic acid dabigatran etexilate is simple in preparation method, excellent in quality and suitable for industrialized production, moreover, has good stability, drug efficacy and security, and is an excellent pharmaceutical form of dabigatran etexilate.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a 1,4-butanedisulfonic acid complex of dabigatran etexilate (Dabigatranetexilate) with anticoagulant effect, a preparation method thereof and a drug combination with the complex as an active ingredient substances, and their use in the preparation of drugs for the prevention or treatment of diseases caused by thrombus or embolism. Background technique [0002] In recent years, the incidence of cardiovascular and cerebrovascular diseases has been on the rise, which has seriously endangered human health. Among them, related diseases caused by thrombus or embolism are the primary factors leading to disability and death. The prevention and treatment of thrombosis and its complications has become an important issue faced by the world medical community. Anticoagulant drugs can effectively improve and prevent cardiovascular and cerebrovascular diseases caused by thrombus, and reduce mort...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07C309/05C07C303/32A61K31/4439A61P7/02
CPCC07D401/12
Inventor 陈洪杜全胜赵永龙徐同利曾琴罗杰向志祥郑伟
Owner 海思科制药(眉山)有限公司
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