58569-36-1

Upstream product

• 551-16-6 6-Aminopenicillanic Acid 
• 40125-73-3 2-sulpho-2-phenylacetyl chloride 
• 39925-38-7 2-phenyl-2-sulfoacetic acid 
• 39925-35-4 2-sulfo-2-phenylacetyl chloride 
• 19460-36-7 triethylammonium 6β-penicillanate 
• 41360-32-1 racemic α-sulfophenylacetic acid 

Downstream Products

• 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%.

Method for preparing D-sulbenicillin sodium

The invention discloses a method for preparing D-sulbenicillin sodium. The method includes steps of removing L-amino acid from L-amino acid salt of D-sulfophenylacetic acid in solvents and carrying out salt forming to obtain D-sulfophenylacetic acid salt; carrying out reaction on the D-sulfophenylacetic acid salt and acylating agents to obtain mixed acid anhydride; dissolving 6-APA in organic solvents under the effect of organic alkali; dropwise adding mixed acid anhydride solution into 6-APA solution, and carrying out sufficient reaction and after-treatment to obtain the D-sulbenicillin sodium. The D-sulfophenylacetic acid is an intermediate. The 6-APA is a matrix. The method has the advantages that the D-sulbenicillin sodium is prepared by the aid of novel synthetic routes, conditions are mild, the method includes stable process and is easy to implement, and the problems of instable processes of existing methods or insufficient optical purity of products and the like can be solved bythe aid of the method.