Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Novel crystal form of dabigatran etexilate mesylate and preparation method of novel crystal form

A dabigatran etexilate methanesulfonate and crystal form technology, applied in the direction of sulfonate preparation, organic chemical methods, chemical instruments and methods, etc., can solve the problems of potential safety hazards, high production costs, and easy residual solvents, etc. Achieve the effects of small dosage, high product yield and high solubility

Inactive Publication Date: 2018-11-23
JIANGSU TASLY DIYI PHARMA CO LTD
View PDF8 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem that the above method exists is that there is a potential safety hazard in the industrial production of acetone, and it is made with p-isopropyl toluene, dimethyl sulfoxide, n-heptane, pyridine, 2-methyltetrahydrofuran, ethyl acetoacetate, 2-butanol, etc. Solvents have the problems of high production cost, easy residue of solvents, and not conventional solvents for industrial production

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Novel crystal form of dabigatran etexilate mesylate and preparation method of novel crystal form
  • Novel crystal form of dabigatran etexilate mesylate and preparation method of novel crystal form
  • Novel crystal form of dabigatran etexilate mesylate and preparation method of novel crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0186] Example 1 Preparation of Dabigatran Etexilate Mesylate Form 1

[0187] Put 20g of dabigatran etexilate mesylate in a reaction flask, add 40ml of dichloromethane, stir and heat to dissolve, add 40ml of ethyl acetate, stir for 15 minutes, cool to 10-15℃, stir and crystallize 1 hour. After filtration, washing with ethyl acetate, and drying, 18.4 g of dabigatran etexilate mesylate crystal form 1 was obtained with a yield of 92%.

Embodiment 2

[0188] Example 2 Preparation of Dabigatran Etexilate Mesylate Form 1

[0189] Put 5g of dabigatran etexilate mesylate in a reaction flask, add 75ml of dichloromethane, stir and heat to dissolve, add 75ml of ethyl acetate, stir for 15 minutes, cool to 10-15°C, stir and crystallize for 1.5 hours . After filtration, washing with ethyl acetate, and drying, 14.1 g of dabigatran etexilate mesylate crystal form was obtained, with a yield of 82.0%.

Embodiment 3

[0190] Example 3 Preparation of Dabigatran Etexilate Mesylate Form 1

[0191] Put 10g of dabigatran etexilate mesylate in a reaction flask, add 80ml of dichloromethane, stir and heat to dissolve, add 100ml of ethyl acetate, stir for 10 minutes, cool to 10-15°C and stir for 1 hour . After filtration, washing with ethyl acetate, and drying, 9.50 g of dabigatran etexilate mesylate crystal form 1 was obtained with a yield of 95.0%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a novel crystal form of dabigatran etexilate mesylate and a preparation method of the novel crystal form. The method comprises the following steps: dissolving dabigatran etexilate mesylate into dichloromethane; and adding tetrahydrofuran to perform recrystallization.

Description

Technical field [0001] The invention belongs to the field of pharmacy, and relates to a crystal form of a pharmaceutical compound, and in particular to a new crystal form of an anticoagulant drug dabigatran etexilate mesylate and a preparation method thereof. Background technique [0002] Dabigatran etexilate mesylate is a new type of direct thrombin inhibitor, a prodrug of dabigatran, and a non-peptide thrombin inhibitor. After oral administration and gastrointestinal absorption, it is transformed into dabigatran with direct anticoagulant activity in the body. Dabigatran binds to the fibrin-specific binding site of thrombin to prevent fibrinogen from cleavage into fibrin, thereby blocking the final step of the coagulation network and thrombosis. Dabigatran can dissociate from the fibrin thrombin conjugate and exert a reversible anticoagulant effect. Its chemical structure is as follows: [0003] [0004] Due to the unique pharmacological activity of dabigatran etexilate mesylat...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D401/12C07C309/04C07C303/32C07C303/44A61K31/4439A61P7/02
CPCC07B2200/13C07D401/12A61K31/4439A61P7/02C07C303/32C07C309/04
Inventor 刘文峥高禹哲王国成刘金平
Owner JIANGSU TASLY DIYI PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com