- 5(1/4) water ceftazidime compound and pharmaceutical composition preparation thereof
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The present invention discloses a 5(1/4) water ceftazidime compound and a pharmaceutical composition preparation thereof, wherein per mole ceftazidime contains 5(1/4) mole water. According to the present invention, the prepared 5(1/4) water ceftazidime compound has good stability and can meet the requirements of the raw material of the preparation.
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Paragraph 0032; 0033; 0038; 0041; 0043
(2019/01/10)
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- One-pot method of preparing Ceftazidime
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The invention relates to a method for preparing ceftazidime by a one-pot process. The method comprises the following steps: by using 7-aminocephalosporanic acid as the raw material, carrying out silanization reaction and iodination reaction, reacting with pyridine, directly adding the liquid into ceftazidime side chain acyl chloride hydrochloride to perform acylation reaction without separation to obtain ceftazidime iodate, adding the liquid into a concentrated hydrochloric acid-water mixed solution to perform deprotection, extracting to stratify, and regulating the pH value of the water phase with an alkaline solution to obtain ceftazidime (6R,7R)-7-[[(2-amino-4-thiazolyl)-[(1-carboxy-1-methylethoxy)imino]acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4,2,0]octyl-2-ene-3-methylpyridine pentahydrate. The method has the advantages of high yield, low cost, mild technological conditions, controllable technical process, high safety and low energy consumption, and is simple to operate.
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- One-pot method for preparing ceftazidime
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The invention discloses a one-pot method for preparing ceftazidime. The one-pot method includes the steps that 7-aminocephalosporanic acid, ceftazidime side chain acyl chloride hydrochloride and pyridine are weighed, placed in an ultrasonic wave reactor and ultrasonically oscillated for 2-3 h at the temperature of minus 18 DEG C-minus 15 DEG C and the power of 750-1000 W, the pH value is adjusted to 4.1-4.2, acetone is added into a reaction solution, and a white solid is separated, washed with cold water at the temperature of 0 DEG C-5 DEG C and dried to obtain ceftazidime. In the method, pyridine serves as an acid-binding agent and a catalyst for an acyl chloride and amidogen reaction, a reactant and reaction solvent, other reagents are not added any more, and the workload of impurity research in the later period of new drug research is greatly reduced. By means of environment-friendly ultrasonic oscillation, after the reaction is completed, the processing process is simple, the long crystal growing process is avoided, and meanwhile the possible influence on product quality by acetone residual amount due to acetone washing after cold water washing is avoided. The yield and the purity are high, and the method is suitable for industrial production.
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Paragraph 0031; 0032
(2016/10/27)
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- IMPROVED PROCESS FOR THE PREPARATION OF CEPHALOSPORIN ANTIBIOTICS
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Abstract The present invention more particularly relates to a process for the preparation of cephalosporin antibiotics of the Formula (I) wherein R1 represents hydrogen, trityl, alkyl like CH3, CRaRbCOORc where Ra and Rb independently represent hydrogen or methyl and Rc represents hydrogen or (C1-C6) alkyl; R2 is carboxylate ion or COORd, where Rd represents hydrogen, ester or a counter ion which forms a salt; R3 represents hydrogen, CH3, CH2OCH3, CH2OCOCH3, CH=CH2, Formula (II).
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Page/Page column 12-13
(2008/06/13)
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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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- Method for producing cephalosporins
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A method for producing cephalosporins 7-substituted with an amino-thiazolylacetic group by reacting 7-ACA or its derivatives having the amino group and the carboxyl protected with reactive derivatives of amino-thiazolylacetic acid.
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- Acylation process for obtaining cephalosporin derivatives
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7β-[2-(2-Tritylaminothiazol-4-yl )-2-(t-butyl-oxycarbonylprop-2-yl )oxyiminoacetamido]-3-pyridinium-methyl-3-cephem-4-carboxylate 1 is obtained via a process comprising N-acylation of 7β-amino-3-pyridinium-methyl-3 -cephem-4-carboxylate 1A with a mixed anhydride of 2-(2-tritylaminothiazol-4-yl)-2-(t-butyloxycarbonyl-prop-2-yl)oxyiminoacetic acid formed with a sulfonic acid halide or phosphoric acid halide, preferably carried out with silylated 1A. The process provides substantial yields of 1 of high purity.
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