Preparation method of fondaparinux sodium

A technology of fondaparinux sodium and solution, which is applied in the field of preparation of fondaparinux sodium, can solve the problems of unfavorable production, low purity of fondaparinux sodium compound, etc., and achieves the advantages of promoting mixing, low price and ensuring high efficiency. Effect

Inactive Publication Date: 2019-01-01
ABA CHEM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Aiming at the deficiencies in the prior art, the present invention provides a method for preparing fondaparinux sodium, which has the advantages of high preparation purity and solves the problem that the prepared fondaparinux sodium compound has a low purity and is not conducive to the production of modern technology. question

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment one: a kind of preparation method of fondaparinux sodium comprises the following steps:

[0027] 1) Take 20 parts of the mixed acid and pour it into the reaction kettle for stirring, heat up to 60°C under stirring, keep the temperature at 60°C and continue stirring for 20 minutes, and keep the above solution for later use. The 20 parts of the mixed acid are specifically concentrated sulfuric acid and Toluenesulfonic acid is formed by mixing one to one, wherein the mass fraction of concentrated sulfuric acid is 80% sulfuric acid aqueous solution;

[0028] 2) Take 10 parts of acetylglucosamine, 20 parts of methanol and 10 parts of alkyl thiophosphate successively and put them into a mixer for thorough mixing, then pass the sub-exchange resin to reflux for 10 hours, and control the reaction temperature at 50°C, and place The above materials are reserved for future use;

[0029] 3) Store the solution prepared in step 1) under a pressure of 0.7 MPa for 10 minutes...

Embodiment 2

[0036] Embodiment two: a kind of preparation method of fondaparinux sodium comprises the following steps:

[0037] 1) Take 30 parts of the mixed acid and pour it into the reaction kettle for stirring, heat up to 60°C under stirring, keep the temperature at 60°C and continue stirring for 20 minutes, and keep the above solution for use. The 30 parts of the mixed acid are specifically concentrated sulfuric acid and Toluenesulfonic acid is formed by mixing one to one, wherein the mass fraction of concentrated sulfuric acid is 80% sulfuric acid aqueous solution;

[0038] 2) Take 20 parts of acetylglucosamine, 23 parts of methanol and 14 parts of alkyl thiophosphate in turn and put them into a mixer for thorough mixing, then pass the sub-exchange resin for reflux reaction for 20 hours, the reaction temperature is controlled at 70 ° C, and the The above materials are reserved for future use;

[0039] 3) Store the solution prepared in step 1) under a pressure of 0.7 MPa for 20 minute...

Embodiment 3

[0046] Embodiment three: a kind of preparation method of fondaparinux sodium comprises the following steps:

[0047] 1) Take 25 parts of the mixed acid and pour it into the reaction kettle for stirring, heat up to 60°C under stirring, keep the temperature at 60°C and continue stirring for 20 minutes, and keep the above solution for later use. The 25 parts of the mixed acid are specifically concentrated sulfuric acid and Toluenesulfonic acid is formed by mixing one to one, wherein the mass fraction of concentrated sulfuric acid is 80% sulfuric acid aqueous solution;

[0048] 2) Take 15 parts of acetylglucosamine, 21.5 parts of methanol and 12 parts of alkyl thiophosphate in turn and put them into a mixer for thorough mixing, then pass the sub-exchange resin to reflux for 15 hours, and control the reaction temperature at 60°C, and The above materials are reserved for future use;

[0049] 3) Store the solution prepared in step 1) under a pressure of 0.7 MPa for 15 minutes, so th...

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Abstract

The invention relates to the technical field of fondaparinux sodium, and discloses a preparation method of fondaparinux sodium. The method comprises the following steps that 20-30 parts of mixed acidis taken, and is poured in a reaction kettle for stirring, at a stirring state, the temperature is increased to 60 DEG C, and then is maintained at 60 DEG C, stirring is continued for 20 min, a solution is left for later use, 10-20 parts of acetyl glucosamine, 20-23 parts of methyl alcohol and 10-14 parts of alkyl thiophosphate are taken in sequence, and are placed in a stirrer for full mixing, through ion exchange resin, reflux reaction is carried out for 10-20 hours, the reaction temperature is controlled at 50-70 DEG C, and a material is left for later use. According to the preparation method of fondaparinux sodium, through sedimentation, high-purity fondaparinux sodium is prepared, in a whole production process, through multiple distillation and separation processes, fondaparinux sodium impurities are removed thoroughly, obtained fondaparinux sodium has higher purity, through a whole vacuum concentration technology, fondaparinux sodium is purer, reaction of various links is carriedout more thoroughly, the production effectiveness is guaranteed, and the high purity of fondaparinux sodium is guaranteed.

Description

technical field [0001] The invention relates to the technical field of preparation of fondaparinux sodium, in particular to a preparation method of fondaparinux sodium. Background technique [0002] Fondaparinux sodium is originally used for patients undergoing major lower limb orthopedic surgery such as hip fracture, major knee surgery or hip replacement, to prevent the occurrence of venous thromboembolic events. The selectivity of fondaparinux sodium and antithrombin After the combination, the conformation of antithrombin changes, and it can be combined with other antithrombin molecules. It has no side effects of thrombocytopenia. It is an excellent anticoagulant drug that does not need to be monitored for clinical application. It has been approved in France, the United Kingdom, and Germany. , China and the United States and other countries, the preclinical data based on conventional safety pharmacology studies, repeated dose toxicity studies and genotoxicity studies did n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/04C07H1/06C07H1/00
CPCC07H1/00C07H1/06C07H15/04
Inventor 徐军蒋信义张敏华周宇徐萌
Owner ABA CHEM CORP
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