- Preparation method of ceftizoxime sodium and preparation method of ceftizoxime sodium intermediate
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The invention belongs to the technical field of medicines, and particularly relates to a preparation method of ceftizoxime sodium and a preparation method of a ceftizoxime sodium intermediate. The preparation method of ceftizoxime sodium comprises the following steps of: adding 7-amino-3-cephalosporin-free 4-carboxylic acid diphenyl methyl ester and (E)- 2-(2-aminothiazole-4-yl)-2-(methoxyimino) acetic acid into a DMF solution, adding a condensing agent, reacting completely, adding water into the reaction solution, filtering to obtain ceftizoxime sodium intermediate filtrate, adding acid to adjust pH, and filtering and drying to obtain ceftizoxime acid; and suspending the ceftizoxime acid in water, adding sodium bicarbonate, adding activated carbon after dissolution of sodium bicarbonate,filtering to obtain filtrate, adding acetone, crystallizing, filtering and drying to obtain ceftizoxime sodium. According to the method, 7-amino-3- cephalosporin-free-4-carboxylic acid diphenyl methylester and (E)-2-(2-aminothiazole-4-yl)-2-(methoxyimino) acetic acid are directly condensed, a diphenyl methyl ester protecting group is removed by a one-step method, the process is safe and environment-friendly, the raw materials are low in price, and the quality of the obtained ceftizoxime sodium is superior to that of the ceftizoxime sodium prepared by the traditional process.
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Paragraph 0037; 0045-0050
(2021/02/06)
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- Synthesis method of ceftizoxime acid
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The invention discloses a synthesis method of ceftizoxime acid, and belongs to the technical field of pharmaceutical synthesis. According to the method, 7-ANCA and AE active ester react, so as to formthe ceftizoxime acid. The synthesis method has the advantages that the method is simple, reaction is easy to operate, the yield and purity are high, and by-products are less, and the method is suitable for industrial production.
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Paragraph 0022-0033
(2019/04/04)
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- A one-head spore zuozuo wo sodium compound (by machine translation)
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The present invention discloses a one-head spore zuozuo wo sodium compound, per mole of ceftizoxime sodium containing 1 mole water. The corresponding X-ray characteristic diffraction peaks of the 2 θ angle of the 11.43 ± 0.2 °, 13 . 24 ± 0.2 °, 16 . 54 ± 0.2 °, 17 . 86 ± 0.2 °, 19 . 45 ± 0.2 °, 20 . 66 ± 0.2 °, 22 . 33 ± 0.2 °, 22 . 88 ± 0.2 °, 23 . 29 ± 0.2 °, 23 . 66 ± 0.2 °, 24 . 59 ± 0.2 ° has a characteristic diffraction peak. The method of the invention by a water head preparation of spore zuozuo wo sodium compound, has good stability and meet the requirements as a raw material of a preparation. (by machine translation)
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Paragraph 0027; 0028; 0034
(2019/01/17)
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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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- 7-[2-(2-Aminothiazol-4-yl)-2-cyclopentyloxyiminoacetamido]-3-cephem-4-carboxylic acid (synisomer)
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The invention relates to new thiadiazolyl or thiazolyl-substituted cephem and cepham compounds, the pharmaceutically acceptable salts and bioprecursors thereof, of antimicrobial activity, processes for preparation thereof, intermediates for preparing the new compounds and to pharmaceutical compositions comprising the new compounds, and methods of using the compositions for treatment of infectious diseases.
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