- Method for synthesizing cephalosporin
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The invention provides a method for synthesizing cephalosporin. The method comprises the following steps that 1, 7-ADCA dissolving liquid is prepared, wherein a solution and 7-ADCA submicron powder are put in a reaction tank, cooling is carried out, at the temperature of 10 DEG C or below, a solvent is added, heat preservation and reacting are carried out, and the 7-ADCA dissolving liquid is obtained; b, N-Phenylglycine potassium salt and pivaloyl chloride react in advance to prepare a mixed anhydride solution; c, the 7-ADCA dissolving liquid prepared in step a is added to the mixed anhydridesolution, a condensation reaction is carried out at the temperature of -40 DEG C to -30 DEG C, and a condensed solution is obtained; d, the condensed solution obtained in step c is subjected to hydrolysis and crystallization, and cephalosporin is obtained. According to the method for synthesizing cephalosporin, the 7-ADCA submicron powder raw material is used, the specific dissolving temperature is adopted in cooperation, the yield of the final cephalosporin product is greatly increased, the purity of the final cephalosporin product is greatly improved, and the method is suitable for industrial popularization and application.
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Paragraph 0018; 0019; 0020; 0021; 0022; 0023; 0024-0032
(2019/04/26)
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- Cefradine compound prepared by adopting high-flux medicine crystal form rapid screening technology and preparation thereof
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The invention discloses a cefradine compound prepared by adopting a high-flux medicine crystal form rapid screening technology. The 'high-end medicine product refined crystallization technology development and industrialization project' won the second prize of the national scientific and technological process in 2015, and the high-flux medicine crystal form rapid screening technology belongs to one of the high-end medicine product refined crystallization technology. The cefradine compound is measured by adopting X-ray powder diffraction, and main characteristic peaks represented by a diffraction angle 2 theta in an atlas are 11.46+/-0.2 degrees, 18.47+/-0.2 degrees, 20.85+/-0.2 degrees, 23.21+/-0.2 degrees and 29.32+/-0.2 degrees. The compound is high in purity, low in impurity content and good in flowability and stability. Meanwhile, the invention discloses a preparation prepared by adopting cefradine, and the preparation is the cefradine for injection. The preparation is simple in preparation process, does not need any excipient, has the better solubility and stability and is smaller in side effect compared with an existing preparation.
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Paragraph 0043; 0044; 0045; 0046; 0047; 0048; 0049
(2017/04/03)
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- SALT OF DIHYDROPHENYLGLYCINE METHYL ESTER
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The present invention relates to the hemi sulfuric acid salt of methyl (R)-2-amino-2-(cyclohexa-1,4-dien-1-yl)acetate, also trivially referred to as the hemi sulfuric acid salt of D-dihydrophenylglycine methyl ester, to a method for the preparation of said salt and to the use of said salt in the enzymatic synthesis of antibiotics.
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- MANUFACTURING METHOD AND APPARATUS OF ULTRAFINE PARTICLES HAVING UNIFORM PARTICLE SIZE DISTRIBUTION
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The present invention relates to a novel technology for forming fine particles with a size of 0.02?3 microns from a solid that can be dissolved in a liquid solvent and is not decomposed by heat. The particle preparation technology according to the present invention may be applicable to the fields of food, cosmetics, biopolymer, polymer compositions, and pharmaceuticals.
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- Synthesis of cephalosporin-type antibiotics by coupling of their β-lactam nucleus and racemic amino acid side chains using a clathration-induced asymmetric transformation
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The cephalosporin-type antibiotics Cephalexin, Cephradine and Cefadroxil have been prepared by coupling of their β-lactam nucleus and racemic amino acid side chain precursors. The initially obtained mixture of cephalosporin epimers is subjected to a clathration-induced asymmetric transformation which results in the epimerization of the epi-cephalosporin into the cephalosporin with the correct diastereomeric configuration.
- Kemperman, Gerardus J.,Zhu, Jie,Klunder, Antonius J. H.,Zwanenburg, Binne
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p. 1817 - 1820
(2007/10/03)
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- Complexes of cephalosporins and carbacephalosporins with parabens
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The invention provides complexes of the formula: STR1 wherein X is chloro, hydrogen, vinyl, or --CH3, Z is CH2 or S; n is 0-5; Y is phenyl or 1,4-cyclohexadien-1-yl; R1 and R2 are hydrogen or hydroxy, with the proviso that R1 and R2 are not both hydrogen and R3 is --COO-, --COO(C1 -C4 alkyl), --NO2 or STR2 wherein R4 is C1 -C4 alkyl.
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- Beta lactam production
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A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a derivative thereof in a halogen-free solvent.
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- Bicyclic beta-lactam/paraben complexes
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The invention provides complexes of the formula: STR1 wherein X is chloro, hydrogen, vinyl, or --CH3, Z is O; is 0-5; Y is phenyl or 1,4-cyclohexadien-1-yl; R1 and R2 are hydrogen or hydroxy, with the proviso that R1 and R2 are not both hydrogen and R3 is --COO-, --COO(C1 -C4 alkyl), --NO2 or STR2 wherein R4 is C1 -C4 alkyl.
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- Synthesis of potential impurities of cefalexin and cefradine
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The synthesis of some impurities of the cephalosporin antibiotics cefalexin and cefradine is described. These impurities which may be present in commercial samples are formed during the semi-synthetic preparation of these antibiotics or upon their degradation. The preparation of these compounds enables the validation of selective quantitative analytical methods, such as column liquid chromatography and thin layer chromatography.
- Hendrix,Roets,Bervoets,Thomas,Pijcke,Busson,Janssen,Hoogmartens
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p. 215 - 219
(2007/10/02)
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- Stable cephradine hydrate
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The invention relates to a novel stable form of cephradine, processes for its production and intermediates used therein.
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- Pharmaceutical tablet, pharmaceutical granulate and process for their preparation
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A pharmaceutical tablet containing an amphoteric beta-lactam antibiotic, microcrystalline or micro fine cellulose or a mixture of both and a second disintegrant, being low-substituted hydroxypropylcellulose, which fully disintegrates in water within 60 seconds. When swallowed it shows a bioavailability as good as a pharmacy prepared suspension of the antibiotic. The tablet is compressed from a mixture containing a new granulate which is prepared from the antibiotic substance, microcrystalline and/or micro fine cellulose and water only. Such tablets can also be prepared by using other known tablet disintegrants as the second disintegrant.
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