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Dabigatran etexilate mesylate anhydrous compound

A technology of ethyl propionate mesylate and ethyl acetate, applied in the field of medicine, can solve the problems of high impurities, moisture absorption and weight gain, difficulty in product purification and the like

Inactive Publication Date: 2015-03-18
TIANJIN HANRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Above-mentioned dabigatran etexilate mesylate method product purification difficulty, dabigatran etexilate makes its mesylate can effectively reduce impurity, purify product, but impurity is still higher, also has certain hygroscopic weight gain

Method used

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  • Dabigatran etexilate mesylate anhydrous compound
  • Dabigatran etexilate mesylate anhydrous compound
  • Dabigatran etexilate mesylate anhydrous compound

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Add 14L tetrahydrofuran and 14L ethyl acetate to the reaction kettle, then add 4.1kg dabigatran etexilate, heat up to 55°C, dissolve, filter, add 28.5L ethyl acetate to the filtrate, keep warm at 55°C, add 626g methanesulfonate dropwise The mixed solution of acid and 7.5L ethyl acetate was added and kept warm and stirred for 1 hour, cooled naturally to room temperature, filtered, and air-dried at 45°C for 5 hours to obtain 4kg of dabigatran etexilate mesylate, with a yield range of 82%- 92%, the chemical purity is as high as 99.9%, the maximum impurity is less than 1‰, and the optical purity is as high as 99.9%ee or more.

[0042] Instrument model and measurement conditions: Rigaku D / max 2500 diffractometer; CuKa, 40Kv, 100mA; 2θ scanning range: 0-50 ° .

[0043]

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a new medicinal crystal form of dabigatran etexilate mesylate. Prepared dabigatran etexilate mesylate disclosed by the invention has the advantages that the chemical purity is 99.9%, the maximum impurity content is less than 0.1%, and the optical purity reaches 99.96%ee; and dabigatran etexilate mesylat is good in stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the anhydrous form of dabigatran etexilate mesylate and a preparation method thereof. The invention also relates to the prevention of diseases such as stroke and systemic embolism in patients with non-valvular atrial fibrillation using the composition of the compound application. Background technique [0002] Atrial fibrillation, abbreviated as atrial fibrillation, is a common cardiovascular disease characterized by irregular heartbeat. The heartbeat of a normal person is 60-100 beats per minute, but in atrial fibrillation, the atrium "vibrates" 350-600 times per minute, and the muscle fibers in the atrium present a rapid and chaotic tremor, thus losing effective contraction ability. When atrial fibrillation occurs, the patient will obviously feel irregular heartbeat, chest tightness, and shortness of breath. Experiments have shown that the incidence of atrial fibr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P9/10A61P7/02
CPCC07D401/12
Inventor 严洁李轩
Owner TIANJIN HANRUI PHARMA
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