- Preparing method of Cefsulodin
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The present invention discloses a Preparing method of Cefsulodin, comprising the steps of Intermediate D-alpha-Sulfophenylacetic acid or its salt with acylating agent to form mixed acid anhydride; Key intermediate 7-PACA dissolved in the solvent in the organic base or inorganic base under the a certain temperature to get 7-PACA solution; dropping mixed acid anhydride solution into 7- PACA solution, and to obtain the Cefsulodin after full reaction and treatment. The method adopts the new synthetic method to carry out the 7-position condensation reaction with the mixed acid anhydride method. The new method has mild condition, stable process and easy operation, which is helpful in solving unstable process problems caused by hard production of Sulfophenylacetyl chloride, unstable Acyl chloride, or the instability of the intermediate in the subsequent reaction.
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Paragraph 0050; 0051; 0052; 0053; 0092; 0093; 0094; 0095
(2017/08/27)
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- Medicinal cefsulodin sodium compound and preparation method thereof
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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.
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