Process for preparing ceftezole sodium

Abstract

The invention relates to a process for preparing ceftezole sodium. The process comprises the following steps: (1) adding N,N-dimethylacetamide or N,N-dimethylformamide and a first part of acetone, adding ceftezole while stirring, and adding purified water or cooled water for injection until ceftezole is completely dissolved; (2) adding medicinal activated carbon, filtering and washing the activated carbon to obtain a reaction solution A; (3) adding a third part of acetone and adding a sodium-forming agent until the solid is completely dissolved; (4) adding medicinal activated carbon, filtering and washing the activated carbon with a fourth part of acetone to obtain a reaction solution B; (5) cooling the reaction solution B to 8-12 DEG C, dropwise adding the reaction solution A into the reaction solution B for carrying out salt formation and crystallization; (6) after the dropwise addition of the reaction solution A is completed, continuously carrying out heat preservation at 8-12 DEG C and stirring for 60-90 minutes; and (7) washing filter cakes with sterilized and filtered acetone and drying at 40-50 DEG C to obtain the sterile ceftezole sodium solid. The process has the advantages of larger batches, simplicity in operation, high yield, good quality and low processing cost, the solvent is simply recovered and the process is suitable for industrial production.

Description

technical field [0001] The invention relates to a preparation process of ceftezole sodium, which belongs to the technical field of medicine and chemical industry. Background technique [0002] Ceftezole sodium, the English name is Ceftezole Sodium, and its chemical name is (6R,7R)-3-[[(1,3,4-thiadiazol-2-yl)sulfur]methyl] 7-[(1H -tetrazol-1-yl)acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt, its molecular formula is C 13 h 11 N 8 NaO 4 S 3 . Its physical and chemical properties: This product is white to light yellow powder or crystalline powder; odorless, hygroscopic. Soluble in water, slightly soluble in methanol, almost insoluble in ethanol and ether. [0003] [0004] Ceftezole Sodium [0005] Ceftezole sodium is a semi-synthetic cephalosporin derivative, and its mechanism of action is to exert antibacterial activity by inhibiting the synthesis of bacterial cell walls. Ceftezole sodium has antibacterial activity against the f...

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Problems solved by technology

[0006] The preparation method of ceftezole sodium has been introduced in domestic patents. Its common disadvantages are that the crystallization solvent system is large and the batch size is small, the steps are too complicated, the product polymer obtained is high, and the related substances (single largest impurity and total miscellaneous) big and other shortcomings

Chinese patent CN201110214204 discloses a preparation method of ceftezole, the crystal system is large, the dissolution process needs to monitor the pH value, and the operation is cumbersome; Chinese patent CN200910144827 discloses a preparation method of ceftezole sodium, the crystal system is large, and the dissolution process requires Monitor pH value, average yield 88.2%

Comprehensive domestic patent document report content, the production of ceftezole sodium mainly adopts the method that adopts ceftezole and salt-forming agent to form salt first in water system and then crystallize or directly use recrystallization, and its operation is loaded down with trivial details, and solvent consumption is big, The output of a single batch is small, the impurities are not easy to remove and the processing cost is high, so it is not an ideal industrial production process

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