79349-82-9Relevant academic research and scientific papers
One-step environment-friendly preparation method of 7-amino-3-vinyl cephalosporanic acid
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Paragraph 0024; 0032-0035; 0037-0039; 0041-0043; 0045-0047, (2020/09/08)
The invention discloses a one-step environment-friendly preparation method of 7-amino-3-vinyl cephalosporanic acid. The method comprises the following steps: A, uniformly mixing an aprotic organic solvent with water, adding D-7-ACA and an alkaline agent A, dissolving, and adding pyridine chlorochromate or Desmatin iodine pyrane; B, adding methyltriphenylphosphonium bromide into an aprotic organicsolvent, dissolving, adding the reaction solution obtained in the previous step, slowly dropwise adding an alkaline agent B, and reacting to obtain a solution containing a target product salt; and C,adjusting the pH value of the reaction system to 3.5-4.5, separating out a solid, filtering, washing and drying to obtain the product. The researched and developed preparation process has the technical advantages of environmental friendliness, high atom utilization rate, few byproducts, high production efficiency, low production cost and the like.
7 - Amino -3 - vinyl cephalosporanic acid preparation method
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Paragraph 0034-0039, (2019/11/13)
The invention belongs to the technical field of medicine synthesis, and especially discloses a method for preparing 7-amino-3-vinyl cephalosporanic acid. The preparation method takes GCLE as an initial raw material, the GCLE and sodium iodide and triphenylphosphine are reacted in a mixing system of an organic solvent and water to generate phosphine salt, a certain amount of alkali lye is added in an organic phase for reacting to generate the corresponding phosphorus ylide, excess free alkali in an organic phase is removed through washing, formaldehyde and ylide are added for a wittig reaction, the organic phase is concentrated to a certain weight, phenol is added for removing carboxyl protection, amino protection is removed, crystallization is carried out to obtain 7-AVCA. The synthesis method does not require a mixing organic solvent, can realize recovery of sodium iodide and formaldehyde, has the advantages of high product yield, good quality, no three wastes generation, and environmental protection, and is suitable for large scale industrial production.
A 7 - amino - 3 - vinyl - 4 - cephalosporanic acid preparation method (by machine translation)
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Paragraph 0021-0022; 0025-0026; 0027-0028; 0029-0032, (2018/01/11)
The invention discloses a 7 - amino - 3 - vinyl - 4 - cephalosporanic acid preparation method, in order to 7 - phenylacetylamino - 3 - vinyl - 4 - cephalosporanic acid-methoxybenzyl ester as the raw material, to solid super strong acid as catalyst, in the alkyl halide, acetate and acetonitrile in the mixed solvent, in the 0 - 50 °C reaction at a temperature of 1 - 10 hours, the reaction is cooled down to the room temperature after treatment to obtain yellow solid, to obtain the target product, solid super strong acid as transition metal modified tin series solid super strong acid; alkyl halide is carbon atom number 1 - 10 of the chlorine; b ester as CH3 COOR, wherein R is a carbon atom number 1 - 10 alkane. This invention adopts the heterogeneous catalysis in a one-pot reaction technology, the use of high activity of the solid acid catalyst for the preparation of 7 - amino - 3 - vinyl - 4 - cephalosporanic acid, this technology is easy to operate, does not corrode the apparatus, three wastes, after treatment is convenient, solid acid can be used repeatedly, is an economic and practical and environmental protection. (by machine translation)
A method for synthesizing spore parent nucleus antibiotiki head
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, (2017/01/02)
The invention belongs to the technical field of synthesis of cephalosporin intermediates and in particular relates to a synthesis method of antibiotic cephalosporin mother nucleus. The synthesis method of the antibiotic cephalosporin mother nucleus comprises the following steps: (1) preparing a reaction liquid I; (2) preparing a reaction liquid II; (3) preparing a compound GVNA; and (4) preparing AVNA. The synthesis method of the antibiotic cephalosporin mother nucleus has the advantages that production cost is low, reaction time is short, recovery rate of the organic solvent is high, secondary utilization is facilitated, and product yield is high.
7-phenylacetylamino-3-vinyl-4- spore olefine acid method for the preparation of P-methoxybenzyl ester
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, (2017/02/17)
The invention discloses a preparation method of 7-phenylacetamido-3-vinyl-4-p-methoxy benzyl ester cefotaximate and belongs to the Chemical medicine field. The preparation method comprises the following steps: carrying out quaternary phosphorization and vinyl reaction at the same time on 7-phenylacetamido-3-chloromethyl-4-p-methoxy benzyl ester cefotaximate (GCLE), sodium iodide, triphenylphosphine and formaldehyde solution in a mixed system of dichloromethane, acetone and water to obtain 7-phenylacetamido-3-vinyl-4-p-methoxy benzyl ester cefotaximate; and removing 7-amino and 4-carboxyl protecting group according to known methods to prepare cefixime and cefdinir nuclear parent 7-AVCA (7-amino-3-vinyl-4-cephalosporanic acid). The aqueous phase comprising sodium iodide and excessive formaldehyde can be repeatedly applied, so that the utilization ratio of sodium iodide is remarkably improved, the production cost is lowered, and the environmental pollution caused by formaldehyde is reduced. The preparation method disclosed by the invention is low in production cost, simple in operating method and suitable for industrialized production and the raw materials are easily available in the preparation process.
An improved and scaleable preparation of 7-amino-3-vinylcephem-4-carboxylic acid
Chao, Mingyong,Hao, Aiyou
experimental part, p. 924 - 927 (2010/04/22)
A practical and efficient multikilogram-scale preparation of 7-amino-3-vinylcephem-4-carboxylic acid (7-AVCA), a key intermediate used in the synthesis of cefixime and cefdinir, is described utilizing /p-methoxybenzyl 7-phenylacetamido-3-chloromethylcephe
