40125-73-3Relevant articles and documents
Preparation method of sulbenicillin sodium
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Paragraph 0074; 0075, (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%.
Preparing method for D(-)-sulbenicillin disodium
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Paragraph 0031; 0032; 0033, (2016/12/01)
The invention provides a preparing method for D(-)-sulbenicillin disodium. The preparing method includes the concrete operation steps that D(-)-sulfophenylacetic acid, dichloroethane and a catalyst dimethylformamide are added into a reaction container, a BTC/C2H4Cl2 solution serves as an acylating chlorination agent, and a dichloroethane solution of D(-)-sulfophenylacetyl chloride is obtained through preparation; D(-)-sulfophenylacetyl chloride and 6-aminopenicillanic acid are prepared into D(-)-sulbenicillin disodium through condensation and refining. The BTC/C2H4Cl2 solution is adopted as the acylating chlorination agent, reaction efficiency is high, the number of side reactions is small, sulfur dioxide pollution is avoided, and the preparing method is of significance in environment-friendly production; acetone and 75% ethyl alcohol are adopted as solvent in the condensation reaction, the pH value is controlled to be seven through trimethylamine, the condensation reaction is carried out at about 10 DEG C, reaction conditions are moderate, the process is simple and easy to operate, the purity and the yield of the obtained D(-)-sulbenicillin disodium are high, and the preparing method is suitable for industrial production.