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A kind of refining method of high-purity ceftaroline axetil

A technology of ceftaroline fexetil and refining method, which is applied in the field of medicine, can solve the problems of undisclosed refining steps of ceftaroline fexaxil imidazolium salt, low purity and yield, difficult to meet the requirements of ceftaroline fexetil pharmacopoeia and industrial preparation requirements, and achieve The process operation is simple and easy, and the effect of high yield

Active Publication Date: 2020-01-10
北京满格医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] It has become an effective method to obtain high-purity ceftaroline axetil by forming a salt from ceftaroline axetil and imidazoles, and then refining the purity of the salt-forming compound to improve the purity of the finished product of ceftaroline axetil. The specific refining steps of imidazole salt of ceftaroline not disclosed, the purity yield of Chinese patent application CN107216353A is relatively low, and it is difficult to meet the pharmacopoeia requirements and industrial preparation requirements of ceftaroline

Method used

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  • A kind of refining method of high-purity ceftaroline axetil

Examples

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Effect test

Embodiment 1

[0028] Add 10g crude ceftaroline benzimidazole salt to 35ml mixed solution (mixed solution is acetone and water, volume ratio 1:1), stir to dissolve, add dropwise methanol about 18ml at 30°C, dropwise rate 2ml / min, Turn on the stirring speed 10r / min and keep it for 1h, turn on the cooling, the cooling rate is 2℃ / h, and stop cooling when the temperature drops to -5℃, continue to stir for 4h, filter, the filter cake is soaked in 10ml methanol at -5℃, filtered under the conditions of room temperature In a tray with a thickness of 1 cm, dried under reduced pressure at 20°C for 5 hours to obtain 9.4 g of a refined product of ceftaroline proxetil benzimidazole salt, with a yield of 94% and a purity of 99.53% by high performance liquid chromatography.

Embodiment 2

[0030] Add 10g crude ceftaroline benzimidazole salt to 45ml mixed solution (mixed solution is acetone and water, volume ratio 1:1), stir to dissolve, add dropwise methanol about 22ml at 30°C at a rate of 2ml / min. Turn on the stirring speed 10r / min and keep it for 1h, turn on the cooling, the cooling rate is 2℃ / h, and stop cooling when it drops to 0℃, continue stirring for 4h, filter, soak the filter cake with 10ml methanol at 0℃, filter by suction, and spread it on the tray at room temperature With a medium thickness of 1 cm and drying under reduced pressure at 20°C for 5 hours, 9.3 g of a refined product of ceftaroline proxetil benzimidazole salt was obtained, with a yield of 93% and a purity of 99.78% by HPLC.

Embodiment 3

[0032] Add 100g crude ceftaroline benzimidazole salt to 400ml mixed solution (mixed solution is acetone and water, volume ratio 1:1), stir to dissolve, add 200ml methanol at 30°C, drop rate 20ml / min, turn on stirring Rotate speed 15r / min, start cooling after 1h, cooling rate is 2℃ / h, stop cooling when it drops to -5℃, keep stirring for 4h, filter, filter cake is soaked in 100ml methanol at -5℃, filtered, and spread on tray at room temperature With a medium thickness of 1 cm, dried under reduced pressure at 20° C. for 5 hours to obtain 94 g of a refined product of ceftaroline pivoxil benzimidazole salt with a yield of 94% and a purity of 99.83% by high performance liquid chromatography.

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Abstract

The invention relates to a refining method of high-purity ceftaroline fosamil, and belongs to the technical field of medicines. The specific technical scheme is that the refining method comprises thefollowing steps: at the temperature of 30 DEG C, adding a ceftaroline fosamil benzimidazole crude product into a mixed solvent and dissolving the ceftaroline fosamil benzimidazole crude product by stirring; stirring the mixture and dropping methanol; cooling, maintaining the same rotation speed, stopping cooling at the temperature of -5 DEG C and continuously stirring the mixture; filtering, soaking a filter cake with -5 DEG C methanol, performing suction filtration, washing the filter cake, spreading the filter cake in a tray at the thickness of 1 cm, and drying the filter cake under reducedpressure at the temperature of 15 DEG C, so as to obtain a ceftaroline fosamil benzimidazole finished product. The refining method is simple, convenient and easy in process operation and high in yield, and therefore, the refining method is suitable for large-scale industrial production.

Description

Technical field: [0001] The invention relates to a method for refining high-purity ceftaroline fosamil, which belongs to the technical field of medicine. Background technique: [0002] Ceftaroline Pivoxil Injection is a kind of cephalosporin antibacterial. The antibacterial principle is to inhibit bacterial cell wall production. It is used to treat adult community-acquired bacterial pneumonia and acute bacterial skin and skin structure infections, including methicillin-resistant golden yellow staphylococcus. The pharmacopoeias of various countries have very high requirements for the purity of APIs, and high-purity APIs are an important foundation for the realization of safe, effective and quality controllable drugs. [0003] Ceftaroline fosamil injection, the active ingredient is: (6R,7R)-7-[(2Z)-2-(ethoxyimino)-2-[5-(phosphoramido)-1,2,4- Thiadiazol-3-yl]-acetyl]-amino]-3-[4-(1-methylpyridine-1- -4-yl)-1,3-thiazol-2-yl]-sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carb...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6561
CPCC07F9/65613
Inventor 于善有彭涛卢作勇汪娟
Owner 北京满格医药科技有限公司