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Preparation method of eltrombopag diethanolamine salt

A technology of ethanolamine salt and ethanolamine is applied in the field of preparation of Eltrombopag diethanolamine salt, and can solve the problems of unsuitability for industrial production, unqualified solvent residue and the like

Inactive Publication Date: 2017-07-21
CHANGZHOU PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The purpose of the present invention is to solve the technical problem of preparing Eltrombopag diethanolamine salt, solvent residue is unqualified, and is not suitable for industrial production

Method used

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  • Preparation method of eltrombopag diethanolamine salt
  • Preparation method of eltrombopag diethanolamine salt
  • Preparation method of eltrombopag diethanolamine salt

Examples

Experimental program
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Embodiment 1

[0022]

[0023] Add Eltrombopag free base (50g, 113mmol) and ethyl acetate 500ml into a reaction bottle and stir at 25±5°C for about 30min, add ethanolamine (69g, 1.13mol), and react at 30±5°C for about 30min , filtered, and the filter cake was dried with hot air at 50±5°C for about 3 hours to obtain 63.2 g of Eltrombopag diethanolamine salt. Yield: 99%, purity: 99.8%, solvent residue: 0.06% (ethyl acetate). The prepared Eltrombopag diethanolamine salt was pulverized according to the preparation requirements. figure 1 Eltrombopag diethanolamine salt XRPD pattern.

Embodiment 2

[0025] Add Eltrombopag free base (50g, 113mmol) and ethyl acetate 500ml into a reaction flask and stir at 25±5°C for about 30min, add ethanolamine (14.5g, 237mmol), heat the reaction to reflux and stir for about 30min, filter , and the filter cake was vacuum-dried at 30±5°C for about 24 hours to obtain 63 g of Eltrombopag diethanolamine salt. Yield: 98.7%, purity: 99.3%, solvent residue: 0.04% (ethyl acetate).

Embodiment 3

[0027] Add Eltrombopag free base (50g, 113mmol) and ethyl acetate 500ml into a reaction bottle and stir at 25±5°C for about 30min, add ethanolamine (138g, 2.26mol), and react at 35±5°C for about 2 hour, filtered, and the filter cake was dried with hot air at 80±5°C for about 1 hour to obtain 63.2 g of Eltrombopag diethanolamine salt. Solvent residue: 0.14% (ethyl acetate).

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Abstract

The invention provides a preparation method of eltrombopag diethanolamine salt; the preparation method is simple to perform and suitable for industrial production; active pharmaceutical ingredients of the eltrombopag diethanolamine salt prepared herein meet provisions in ICH (international council for harmonisation) guidelines.

Description

technical field [0001] The invention belongs to the technical field of preparation of eltrombopag diethanolamine salt. Background technique [0002] On November 20, 2008, the US FDA approved GlaxoSmithKline's Eltrombopag tablets (Promacta) for the treatment of chronic idiopathic platelets after glucocorticoids, immunoglobulin therapy or splenectomy. Thrombocytopenia in patients with ITP. [0003] Eltrombopag is the first oral non-peptide thrombopoietin receptor agonist approved for the treatment of adults with chronic ITP. Preclinical and clinical studies have shown that stimulating this product can increase the proliferation and differentiation of platelet-derived bone marrow megakaryocytes. Its approval for the treatment of ITP patients is an important milestone. [0004] Eltrombopag diethanolamine salt chemical name: 3'-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo -4H-pyrazole-4-ylidene]hydrazino]-2'-hydroxyl-[1,1'-biphenyl]-3-carboxylic acid di-(monoethano...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/46
CPCC07D231/46
Inventor 郭乙杰巫美金
Owner CHANGZHOU PHARMA FACTORY
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