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A cefuroxime sodium and synthetic method technology, applied in the field of drug synthesis, can solve problems such as high production cost, β-lactam ring damage, and reduced yield, and achieve stable product quality, simplified production steps, and reduced production costs. Effect
Active Publication Date: 2009-12-30
哈药集团股份有限公司 +1
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[0007] The above-mentioned process method has been applied by most manufacturers at home and abroad, and has reached a relatively stable production level, but in the first step, hydrolysis under strong alkali conditions will cause great damage to the β-lactam ring, which will not only reduce the yield , It also has a great impact on the stability of product quality, resulting in unstable color grades, reduced content, and high production costs.
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Embodiment 1
[0034] Preparation of MDCC (decarbamoylcefuroxime acid):
[0035] In a 1000ml dry four-neck bottle, add 220ml of dichloromethane, PCI 5 35g, stir quickly for 1 hour, lower the temperature to -30°C, add 48ml of DMA (N.N-dimethylacetamide), 26g of SMIA, -10~-12°C, react for 80 minutes, wash with 3×110mil purified water, separate two Chloromethane phase is ready for use.
[0036] In another 250ml four-neck bottle, add 132ml of purified water, add 25.4g of 7-DACA, 0~2°C, dissolve until clear with 15% sodium hydroxide, add the above dichloromethane phase twice (previously Pour into the dissolved solution, keep the pH 6.5-7.0, react for 2 hours, separate the water phase, add 36ml of purified water to extract once, combine the water phase, when the temperature reaches 5-10°C, add 0.16g of disodium EDTA, 0.3g of sodium metabisulfite and 150ml of dichloromethane, then use 52ml of 16% hydrochloric acid to adjust the pH of the feed solution to 2.0, stir for 30 minutes and then filter, ...
Embodiment 2
[0042] Method is with embodiment 1,
[0043] Wherein water and dichloromethane mixed solvent are volume ratio 100ml: 200ml, adjust pH value to 1 with hydrochloric acid; Sodium bicarbonate lye is 1% sodium bicarbonate lye, absolute ethanol and acetone mixed solvent are volume ratio 2: 1.
Embodiment 3
[0045] Method is with embodiment 1,
[0046] Wherein water and dichloromethane mixed solvent are volume ratio 500ml: 100ml, adjust pH value to 2 with hydrochloric acid; Sodium bicarbonate lye is 10% sodium bicarbonate lye, absolute ethanol and acetone mixed solvent are volume ratio 1: 2.
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Abstract
The invention relates to a method for synthesizing cefuroxime sodium, which comprises the following steps: 1, performing the N- acylation reaction of 3-deacetyl-7aminocephalosporanic acid and methoxyaminofuranyl ammonium salt which serve as raw materials and adjusting the pH value with hydrochloric acid to less than 7 in a mixed solvent phase to precipitate crystals to obtain 3-deoxyformyl cefuroxime acid; 2, performing the addition reaction of the 3-deoxyformyl cefuroxime acid and chlorosulfonyl isocyanate serving as a strong ammonia formylating agent in an organic solvent to obtain chlorosulfonyl cefuroxime acid, dehydrating the chlorosulfonyl cefuroxime acid to obtain the cefuroxime acid, decarburizing and concentrating the cefuroxime acid, crystallizing the cefuroxime acid in a solvent phase, and drying the crystals under vacuum to obtain a solid product of cefuroxime acid; and 3, dissolving the cefuroxime acid in alkaline solution, decarburizing the resulting product, crystallizing the resulting product in a mixed solvent phase, filtering crystals, and drying the crystals under vacuum to obtain the cefuroxime sodium.
Description
technical field [0001] The invention relates to a drug synthesis method, in particular to a novel chemical synthesis method of the antibiotic cefuroxime sodium. technical background [0002] There are more than 50 types of cephalosporin antibiotics on the market from the first generation to the fourth generation. The cefuroxime series belongs to the second generation cephalosporins, which have broad-spectrum antibacterial effect and have strong antibacterial effect on the hydrolytic enzymes produced by bacteria that destroy the drug effect. High stability ensures excellent antibacterial activity, rarely adverse reactions in clinical application, and has excellent curative effect on most infections caused by β-lactamase-producing pathogenic bacteria. Cefuroxime sodium was first developed and marketed by the British Glaxo (Glaxo) company in 1975, and listed in the United States in 1988. After the patent protection expired in 1996, it was still the best in the β-lactam anti-inf...
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