- Cefotaxime sodium pharmaceutical preparation, and application thereof in treatment of new salmonella infection indications including typhoid and paratyphoid
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The invention provides a cefotaxime sodium, and a preparation method, a cefotaxime sodium preparation and application thereof. The mass content of the cefotaxime sodium is 98% or above, and the cefotaxime sodium also comprises impurities A, B and C. The preparation method comprises the following steps: firstly, reacting methoxyiminoacetic acid with an activating agent to obtain an active ester intermediate; reacting 7-ACA with the active ester intermediate under a temperature control condition, and performing acid regulation and crystallization to obtain cefotaxime acid; carrying out a salifying reaction on cefotaxime acid and a salifying agent in a salifying solvent, and separating out to obtain the cefotaxime sodium. The cefotaxime sodium is low in impurity content, beneficial to long-term storage and placement, good in quality stability and better in clinical curative effect and safety, and can be used for treating salmonella infections including typhoid and paratyphoid.
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- Cefotaxime sodium preparation method
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The invention provides a cefotaxime sodium preparation method. The method is characterized in that after an active group of 7-aminocephalosporanic acid is protected by a silanization reagent, subjecting to condensation reaction with AE-active ester to generate cefotaxime acid containing a protecting group; after deprotection of the cefotaxime acid containing the protecting group under the action of a deprotection agent, sequentially subjecting to aqueous-phase acidification and crystallization to obtain cefotaxime acid; subjecting the cefotaxime acid to salification and solvent crystallizationto obtain a pure product of cefotaxime sodium. In a whole technical process, a product degradation process is reduced, product quality is evidently improved, product market competitiveness is improved, and medication safety is further guaranteed.
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Paragraph 0071-0073; 0078-0080; 0085-0087
(2019/04/17)
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- 1/4 water cefotaxime sodium compound
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The invention discloses a 1/4 water cefotaxime sodium compound and a preparation method thereof. The cefotaxime sodium per mole contains 1/4 mole of water. The 1/4 water cefotaxime sodium compound obtained has good particle size distribution, good fluidity, low impurity content, thermodynamic stability and wide application prospects.
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Paragraph 0035; 0044; 0053
(2019/01/17)
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- Cefotaxime sodium compound prepared by fluid mechanics principle and preparation of cefotaxime sodium compound
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The invention discloses a cefotaxime sodium compound prepared by the fluid mechanics principle and a preparation of the cefotaxime sodium compound, namely efotaxime sodium for injection. A 'research, development and industrialization project of high-end medicine product refining and crystalizing technologies' acquires the second prize of 2015 National Science and Technology Progress Award, and the fluid mechanics principle belongs to one of the high-end medicine product refining and crystalizing technologies. The cefotaxime sodium compound is measured by X-ray powder diffraction, and the main feature peaks indicated by diffraction angles 2theta in the spectrum of the cefotaxime sodium compound is 9.24 degrees, 18.65 degrees, 20.65 degrees, 25.10 degrees and 28.42 degrees. The cefotaxime sodium compound is high in purity, low in impurity content, good in flowability and good in stability.
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Paragraph 0051; 0052; 0053
(2017/04/28)
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- Synthesis method of cefotaxime sodium
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The invention relates to a synthesis method of cefotaxime sodium. The method includes the steps that with an acetone-water solution as a solvent, 7-ACA and AE-active ester are subjected to a stirring reaction for 5-15 min; then, a sodium hydroxide solution is added with stirring for a reaction, obtained reaction liquor is filtered and then crystallized with acetone, and the product cefotaxime sodium is obtained. By the adoption of the one-step synthesis method, the reaction yield is high, product quality is stable, and the operation process is simple and convenient; moreover, no amine intermediate reactant or cosolvent is used, so that production safety is high.
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Paragraph 0025; 0026; 0027; 0028; 0029; 0030; 0031-0033
(2016/10/27)
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- A method for preparing Cefotaxime
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The invention discloses a preparation method of cefotaxime sodium. Ceftizoxime acid used as the initial raw material reacts with anhydrous sodium acetate to generate the cefotaxime sodium. In such process, purified water, butanol and acetone are selected as crystallizing solvents to control the mixing speed and crystallization temperature in the crystallization process, so that the finally obtained cefotaxime sodium has favorable flowability and can satisfy the subpackaging requirements in production. Various quality indexes of the obtained cefotaxime sodium conform to the requirements for medicinal standard, and thus, the cefotaxime sodium can satisfy the demands for clinical application.
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Paragraph 0030; 0031
(2017/06/20)
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- PROCESS FOR PREPARATION OF CEFOTAXIME ACID AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
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A process for the preparation of cefotaxime acid of formula (IV) and pharmaceutically acceptable salt thereof, such as cefotaxime sodium of formula (I) is provided, which comprises condensing the compound of formula (II) with the compound of formula (III) and using aqueous glyme or aqueous cellosolve as the solvent.
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Page/Page column 9
(2011/04/26)
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- Process for the production of cefotaxime sodium
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A process for the production of 7-[2-(2-amino-4-thiazolyl)-2-syn-methoxyimino-acetamido]-3-acetoxymethyl-3-cephem-4-carboxylic acid (Cefotaxime) in aqueous isopropyl alcohol is provided. The synthesis provides the product in greater than 99 % HPLC purity.
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Page/Page column 4
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF CEPHEM CARBOXYLIC ACIDS
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The invention relates to processes for the preparation of cephem carboxylic acids. More particularly, it relates to the preparation of ceftriaxone and cefotaxime and pharmaceutical compositions that include the ceftriaxone and cefotaxime.
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Page/Page column 11
(2010/02/11)
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- Process for preparing cephalosporins with salified intermediate
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Cephalosporins may be conveniently prepared by a process in which 7-ACA is silylated, acylated, desilylated and then salified to give an intermediate which is eventually cyclized with thiourea.
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Page/Page column 6
(2010/02/11)
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- NOVEL INTERMEDIATES FOR SYNTHESIS OF CEPHALOSPORINS AND PROCESS FOR PREPARATION OF SUCH INTERMEDIATES
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A novel 4-halo-2-oxyimino-3-oxo butyric acid-N, N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics, wherein X is chlorine or bromine; R is hydrogen, C1-4 alkyl group, an easily removable hydroxyl protective group, -CH2COOR5, or -C(CH3)2COOR5, wherein R5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV1), wherein X, R and R5 are as defined above, with N, N-dimethylformiminium chloride chlorosulphate of formula (VII), in an organic solvent at a temperature ranging from -30 °C to -15 °C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.
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- PROCESS FOR THE PREPARATION OF CEFOTAXIME SODIUM
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An improved process for the preparation of the sterile cefotaxime sodium of formula (I), from the compound of formula (II).
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- A rapid procedure to prepare cefotaxime
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A rapid procedure is reported for the synthesis of cefotaxime, by acylation of the 7-amino cephalosporanic acid with the 2- mercaptobenzothiazolyl thioester of (Z)-2-[2-aminothiazol-4-yl]-2- methoxyimino acetic acid (MAEM) that is a commercial reagent. The reaction was carried out at room temperature for 1 h, obtaining 95% yield. 2- Mercaptobenzothiazole was recovered as a side-product with a high purity and yield. The proposed method differentiates from those reported previously for a shorter time and very mild reaction condition, as well as for a ready for use reagent. (C) 2000 Elsevier Science S.A.
- Rodriguez, Juan C.,Hernandez, Ricardo,Gonzalez, Maritza,Lopez, Miguel A.,Fini, Adamo
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p. 393 - 396
(2007/10/03)
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- Production of cefotaxime and new sodium salts
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A process for the production of cefotaxime in acetone/water and its use in the production of a sodium salt of cefotaxime and a crystalline sodium salt of cefotaxime in the form of rounded agglomerates and in the form of needles.
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- Dimethyl formiminium chloride chlorosulphate derivatives useful as intermediates for producing cephalosporins
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This invention relates to reactive derivatives of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid and 1H-tetrazol-1-acetic acid of the following general formula I, STR1 wherein R3 = STR2 as well as to use thereof in the manufacture of cephalosporin antibiotics such as cefotaxime, ceftriaxone and cefazolin.
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- Method for manufacture of cephalosporins and intermediates thereof
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This invention relates to reactive derivatives of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetic acid and 1H-tetrazol-1-acetic acid of the following general formula I, whereinR3= as well as to use thereof in the manufacture of cephalosporin antibiotics such as cefotaxime, ceftriaxone and cefazolin.
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- Process for separation of syn and anti oxime isomers of cephalosporin-compounds
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A process for the separation of a mixture of syn and anti oxime isomers one from the other which comprises adsorbing said mixed oxime isomers onto a non-functional macroreticular adsorption resin, and eluting said resin to yield at least one eluate fraction containing one of said isomers while being substantially free of the other of said isomers. The application of this process to the separation of syn and anti isomers of cephalosporin compounds possessing an oxime grouping in a side-chain in the 7β-position, and of acids corresponding to this 7β-side chain, is described.
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