39925-35-4Relevant academic research and scientific papers
Preparation method of sulbenicillin sodium
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Paragraph 0058; 0062; 0070, (2018/09/08)
The invention discloses a preparation method of sulbenicillin sodium. According to the invention, L-amino acid is firstly adopted to perform splitting on D, L-sulfonylphenylacetic acid to obtain D(-)-sulfonylphenylacetic acid, then D(-)-sulfonylphenylacetic acid is compounded with D, L-sulfonylphenylacetic acid to prepare a sulfonylphenylacetic acid mixture with D(-)-sulfonylphenylacetic acid to L(+)-sulfonylphenylacetic acid ratio being about 78%:22%, the sulfonylphenylacetic acid mixture is chlorinated and then reacts with 6-APA, and then reacts with sodium iso-octoate, to directly obtain asulbenicillin sodium mixture with the ratio of D(-)-sulbenicillin sodium to L(+)-sulbenicillin sodium being about 78%:22%. According to the invention, post-treatment process is simplified, no water isused in the step of producing sulbenicillin sodium, hydrolysis impurity level is reduced, product purity is more than 99.0%, and product mole rate is more than 90%.
Medicinal cefsulodin sodium compound and preparation method thereof
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Paragraph 0051; 0052; 0053; 0054; 0055; 0056; 0057; 0058, (2017/07/21)
The invention relates to the technical field of medicine, in particular to a medicinal cefsulodin sodium compound and a preparation method thereof. The preparation method of the medicinal cefsulodin sodium compound includes steps: 1) preparation of 3-(4-pyridinecarboxamide-1-methylene)-7-amino-cephalosporanic acid; 2) preparation of D-sulfophenylacetyl chloride; 3) preparation of D-sulfocephalosporanic acid; 4) preparation of cefsulodin sodium. The technical defects of high cost, low safety and low yield of existing preparation methods are overcome; by adoption of a silicon reagent method for preparation of the cefsulodin sodium compound, racemate controllability, high safety, high yield and high quality are realized, starting materials are easy to acquire, reaction conditions of each step are mild, equipment requirements are low, a single solvent is adopted and convenient to recycle, the requirement on environment friendliness can be met, and the method is suitable for large-scale industrial production.
