Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of eltrombopag

A technology of solution and glass dish, which is applied in the field of Eltrombopag preparation, can solve the problems affecting the quality of drug testing and long preparation process, and achieve the effects of increasing the preparation speed, accelerating the chemical reaction process, and shortening the preparation time

Inactive Publication Date: 2018-12-28
ABA CHEM SHANGHAI
View PDF4 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies of the prior art, the present invention provides a preparation method of Eltrombopag, which has the advantages of high-efficiency preparation process and more environmental protection, and solves the problem of the preparation of the drug Eltrombopag, wherein the raw materials used in the chemical reaction are reduced There are some highly toxic materials that do not dissipate during the reaction process, which will still affect the quality of drug testing, and the preparation process is relatively long.

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment one: a kind of preparation method of Eltrombopag comprises the following steps:

[0022] 1) Take 12% of 2-nitro-6-bromophenol, 5% of potassium carbonate and 7% of benzyl bromide successively, pour into 120ml of acetonitrile solution to carry out reflux reaction, heat up the reflux reaction to 90°C and keep the temperature at 90°C After continuing to reflux for 3 hours, the reflux device was cooled to room temperature, the resulting solution was filtered and concentrated to a dry solid, and the solid was put into a 100ml glass dish, and 40ml of triethylamine liquid was added, and the glass dish was continuously heated. After white crystals appear on the surface of the solid, cool down the glass dish, wash and filter the solid with clean water, and keep the above materials for later use;

[0023] 2) adding 100ml of ethyl acetate to the material obtained in step 1) for dissolving, washing with 50ml of water and 50ml of saturated sodium chloride solution successi...

Embodiment 2

[0028] Embodiment two: a kind of preparation method of Eltrombopag comprises the following steps:

[0029] 1) Take 16% of 2-nitro-6-bromophenol, 6.25% of potassium carbonate and 11% of benzyl bromide successively, pour into 120ml of acetonitrile solution to carry out reflux reaction, and keep the temperature at 90°C after the reflux reaction is heated to 90°C After continuing to reflux for 3 hours, the reflux device was cooled to room temperature, the resulting solution was filtered and concentrated to a dry solid, and the solid was put into a 100ml glass dish, and 40ml of triethylamine liquid was added, and the glass dish was continuously heated. After white crystals appear on the surface of the solid, cool down the glass dish, wash and filter the solid with clean water, and keep the above materials for later use;

[0030] 2) adding 100ml of ethyl acetate to the material obtained in step 1) for dissolving, washing with 50ml of water and 50ml of saturated sodium chloride solut...

Embodiment 3

[0035] Embodiment three: a kind of preparation method of Eltrombopag comprises the following steps:

[0036] 1) Take 20% of 2-nitro-6-bromophenol, 7.5% of potassium carbonate and 15% of benzyl bromide successively, pour them into 120ml of acetonitrile solution to carry out reflux reaction, heat up the reflux reaction to 90°C and keep the temperature at 90°C After continuing to reflux for 3 hours, the reflux device was cooled to room temperature, the resulting solution was filtered and concentrated to a dry solid, and the solid was put into a 100ml glass dish, and 40ml of triethylamine liquid was added, and the glass dish was continuously heated. After white crystals appear on the surface of the solid, cool down the glass dish, wash and filter the solid with clean water, and keep the above materials for later use;

[0037] 2) adding 100ml of ethyl acetate to the material obtained in step 1) for dissolving, washing with 50ml of water and 50ml of saturated sodium chloride solutio...

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 relates to the technical field of pharmaceutical manufacturing and discloses a preparation method of eltrombopag. The method comprises the following steps: 1) 12%-20% of 2-bromo-6-nitrophenol, 5%-7.5% of potassium carbonate and 7%-15% of benzyl bromide are taken sequentially and poured into 120 ml of an acetonitrile solution for a reflux reaction, temperature is increased to 90 DEG Cfor the reflux reaction and kept at 90 DEG C for continuous reflux for 3 h, then a reflux device is cooled to room temperature, an obtained solution is filtered and concentrated, dry solids are obtained and placed into a 100ml glass dish, and 40 ml of a triethylamine liquid is added. According to the preparation method of eltrombopag, the triethylamine liquid is added to the solids prepared in step 1, the triethylamine liquid and benzyl bromide can be subjected to a chemical reaction, white crystals of quaternary ammonium are generated by the reaction, the white crystals can be washed by clear water, so that benzyl bromide in the solids is eliminated, toxin components of the drug are reduced, follow-up manufacture of the drug is facilitated, product quality is guaranteed, and competitiveness of an enterprise is enhanced.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical manufacturing, in particular to a preparation method of Eltrombopag. Background technique [0002] Eltrombopag is an oral thrombopoietin drug developed by GlaxoSmithKline. It is a small molecule thrombopoietin receptor agonist. It can interact with the thrombopoietin receptor in the transmembrane region of the human body to generate signal levels Combined amplification effect, thereby inducing the proliferation and differentiation of bone marrow megakaryocytes, the drug was approved by the US Food and Drug Administration (FDA) for marketing in the United States in November 2008, and is used to treat glucocorticoids and immunoglobulins. or thrombocytopenia in patients with chronic idiopathic thrombocytopenic purpura (ITP) after splenectomy, Eltrombopag is the first oral non-peptide thrombopoietin receptor agonist approved for the treatment of adults with chronic ITP, and it is approved for t...

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
Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/46
CPCC07D231/46
Inventor 徐军蒋信义张敏华周宇徐萌
Owner ABA CHEM SHANGHAI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap 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