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Method for preparing ceftriaxone sodium

A technology of ceftriaxone sodium and aminocephalosporanic acid, applied in the direction of organic chemistry, etc., can solve the problems of increasing the difficulty of solvent recovery, increasing the cost of producing ceftriaxone, and high toxicity

Active Publication Date: 2014-01-29
珠海保税区丽珠合成制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0016] The synthetic routes reported by the above-mentioned patent process are basically similar, either using a single solvent with high toxicity, such as methanol, dichloromethane; or using a ternary mixed system, such as ethanol, dichloromethane and water; or using a binary solvent, Such as tetrahydrofuran and water; the reported synthesis processes have all adopted solvents that are harmful to the environment or humans, and if a mixed organic system is used, it will increase the difficulty of solvent recovery, thereby increasing the cost of producing ceftriaxone

Method used

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  • Method for preparing ceftriaxone sodium
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  • Method for preparing ceftriaxone sodium

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Embodiment 1: Preparation of 7-ACT

[0035] In a 1000ml three-necked flask, add in sequence: dimethyl carbonate (200ml), 7-ACA (35g, 128.5mmol), TTZ (20.5g, 128.8mmol), EDTANa 2 (0.4g, 1.2mmol) and boron trifluoride-dimethyl carbonate solution (188ml, 493.1mmol) (20% by mass), stirred and reacted for 40 minutes, and the temperature was controlled at T=30°C. After the reaction is completed, cool down to T3 ) hydrolysis to terminate the reaction, then dropwise add 5% ammonia water to seed the crystal until the system becomes turbid, and slowly stir to grow the crystal for 40 minutes. Then continue to drop 5% ammonia water to adjust the pH of the system to 3.8-4.0. After the adjustment is completed, slowly stir and grow the crystal for 30 minutes, and control the temperature T=6-7°C. Suction filtration, suction drying, the filter cake was washed with 40ml acetonitrile + 40ml water for the first wash, washed with 90ml acetone for the second wash, and dried in vacuum, and d...

Embodiment 2

[0036] Embodiment 2: Preparation of 7-ACT

[0037] In a 1000ml three-necked flask, add in sequence: dimethyl carbonate (200ml), 7-ACA (35g, 128.5mmol), TTZ (20.5g, 128.8mmol), EDTANa 2 (0.4g, 1.2mmol) and boron trifluoride-dimethyl carbonate solution (188ml, 493.1mmol) (20% by mass), stirred and reacted for 50 minutes, and the temperature was controlled at T=30°C. After the reaction is completed, cool down to T3 ) hydrolysis to terminate the reaction, then dropwise add 5% ammonia water to seed the crystal until the system becomes turbid, and slowly stir to grow the crystal for 40min. Then continue to drop 5% ammonia water to adjust the pH of the system to 3.8-4.0. After the adjustment is completed, slowly stir and grow the crystal for 30 minutes, and control the temperature T=6-7°C. Suction filtration, suction drying, the filter cake was washed with 40ml of acetonitrile + 40ml of water for the first wash, washed with 90ml of acetone for the second wash, dried in vacuum, and d...

Embodiment 3

[0038] Embodiment 3: Preparation of 7-ACT

[0039] In a 1000ml three-necked flask, add in sequence: dimethyl carbonate (200ml), 7-ACA (35g, 128.5mmol), TTZ (20.5g, 128.8mmol), EDTANa 2 (0.4g, 1.2mmol) and boron trifluoride-dimethyl carbonate solution (188ml, 493.1mmol) (20% by mass), stirred and reacted for 60 minutes, and the temperature was controlled at T=30°C. After the reaction is completed, cool down to T3 ) hydrolysis to terminate the reaction, then dropwise add 5% ammonia water to seed the crystal until the system becomes turbid, and slowly stir to grow the crystal for 40 minutes. Then continue to drop 5% ammonia water to adjust the pH of the system to 3.8-4.0. After the adjustment is completed, slowly stir and grow the crystal for 30 minutes, and control the temperature T=6-7°C. Suction filtration and suction drying, the filter cake was washed with 40ml of acetonitrile + 40ml of water for the first wash, washed with 90ml of acetone for the second wash, and then dried...

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Abstract

The invention relates to a novel green low-cost method for synthesizing ceftriaxone sodium. Firstly, in the 7-ACT synthesis process, the dimethyl carbonate is used as the reaction solvent, and the boron trifluoride-dimethyl carbonate is used as the catalyst, thereby substituting the use of the high-cost high-toxicity acetonitrile; and secondly, in the ceftriaxone sodium synthesis process, the ethanol-water reaction system is adopted to obtain the high-yield high-quality ceftriaxone sodium.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a preparation method of ceftriaxone sodium. Background technique [0002] Ceftriaxone Sodium (Ceftriaxone Sodium, structural formula 1, referred to as CTR), the chemical name is (6R, 7R)-7-[(Z)-2-amino-4thiazolyl)-2(methoxyiminoacetamido] -8-Oxo-5-thio-1aza[4,2,0]-oct-2-ene-2-carboxylic acid disodium salt, the structural formula is as follows: [0003] [0004] Ceftriaxone sodium is a long-acting antibiotic drug among the third-generation cephalosporins. It has a bactericidal effect on many Gram-positive bacteria, negative bacteria and anaerobic bacteria, and it is effective on most of the β-lactamase produced by bacteria Highly stable, thus enhancing its antibacterial effect. Clinically, it is widely used in respiratory tract infection and urinary system infection sensitive to this product, including pyelonephritis and gonorrhea, meningitis, burn infection, postoperative...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/06
CPCC07D501/06C07D501/36
Inventor 张鹏王建军肖鸿江跃江晓漫
Owner 珠海保税区丽珠合成制药有限公司
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