Method for preparing dabigatran etexilate hydrolysis impurities

A technology of dabigatran etexilate and impurities, applied in the field of preparation of dabigatran etexilate hydrolyzed impurities, to achieve the effect of high purity
CN104356111AActive Publication Date: 2015-02-18BENGBU BBCA MEDICINE SCI DEV
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
BENGBU BBCA MEDICINE SCI DEV
Publication Date
2015-02-18

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Abstract

The invention provides a method for preparing a dabigatran etexilate hydrolysis impurity A. The method comprises steps as follows: (1) dabigatran etexilate or dabigatran etexilate mesylate is used as a raw material and dissolved in a mixed medium of an organic solvent and an alkaline aqueous solution for a hydrolysis reaction; (2) a mixed liquid obtained in Step (1) is adjusted to be acidic, and grease is separated out; (3) the organic solvent is added to the grease, crystals are separated out, and the impurity A is obtained. The invention further provides a method for preparing a dabigatran etexilate hydrolysis impurity B. The method comprises steps as follows: (1) the dabigatran etexilate hydrolysis impurity A is used as a raw material and dissolved in a mixed medium of the organic solvent and an acidic aqueous solution for a hydrolysis reaction; (2) a mixed liquid obtained in Step (1) is depressurized and distilled until grease is produced, and extraction is performed with dichloromethane; (3) an obtained extraction liquid is purified with medium-pressure preparation chromatography, the solvent is removed, and the grease is obtained; (4) ethyl acetate is added, crystals are separated out after dissolution, and the impurity B is obtained.
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Description

Technical field

[0001] The invention relates to the quality control of dabigatran etexilate, in particular to a method for preparing dabigatran etexilate hydrolyzed impurities. Background technique

[0002] Dabigatran etexilate mesylate is an oral thrombin inhibitor, its chemical structure is:

[0003]

[0004] Its preparation, dabigatran etexilate capsules, obtained marketing approval in Europe in March 2008, becoming the first new class of oral anticoagulant drug to be marketed in more than 50 years after warfarin. Dabigatran etexilate can be converted into dabigatran in the body, which can inhibit thrombin activity to achieve anticoagulant effect. The drug is mainly used for postoperative venous thromboembolism and specific patient populations. The launch of the drug is a major advance in the field of anticoagulation therapy and the prevention of potentially fatal thrombosis, and is another blockbuster rookie in the field of cardiovascular therapy.

[0005] At present, the pharm...

Claims

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