40125-73-3

Upstream product

• 103-82-2 phenylacetic acid 
• 41360-32-1 racemic α-sulfophenylacetic acid 

Downstream Products

• 39681-08-8 (6R)-3-acetoxymethyl-8-oxo-7t-((Ξ)-2-phenyl-2-sulfo-acetylamino)-(6rH)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid 
• 1345689-71-5 C₅₈H₅₈ClN₄O₁₂S₂⁽¹⁺⁾*I^(1-) 
• 28002-18-8 (2S,5R,6R)-3,3-dimethyl-6-(2-phenyl-2-sulfoacetylamino)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid disodium salt 

Relevant academic research and scientific papers

Preparation method of sulbenicillin sodium

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%.

To facilitate the industrial production of synthesis method of sulbenicillin sodium (by machine translation)

The invention discloses a method of easy industrial production sulbenicillin sodium synthetic method, comprises the following steps: (1) sulfonation reaction; (2) alkalization reaction; (3) ion exchange; (4) chloro acylation reaction; (5) extracting sulphur benzene acetyl chloride; (6) preparation of (-) - α - D - sulbenicillin; (7) the preparation of (-) - α - D - sulbenicillin sodium. The invention relates to a convenient industrial production of synthetic method of sulbenicillin sodium, through reasonable synthetic route design, simplifies the sulphur benzene acetic acid disodium salt of the tedious operation, improves the yield; direct the synthetic process for preparing optically pure (-) - α - D - of sulbenicillin, saves the cost, more favorable to the industrialized production, market prospect. (by machine translation)

Preparing method for D(-)-sulbenicillin disodium

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.

NOVEL CEPHEM DERIVATIVE

Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical composition comprising the same. A Compound of the f