Synthesis method for 2- methoxyl-4-amino-5-ethylsulfonylbenzoic acid

Through a series of compound reactions and protection steps, the problems of expensive reaction raw materials, hazardous solvents and cumbersome steps in the synthesis of 2-methoxy-4-amino-5-ethylsulfonylbenzoic acid are solved, and efficient and safe product synthesis is achieved. , suitable for industrial production.

CN101628886BActive Publication Date: 2012-12-12BEIJING WISTA PHARMA CO LTD
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Patent Information

Application Number
CN200910169328.5
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2009-08-25
Publication Date
2012-12-12
Estimated Expiration
2029-08-25

AI Technical Summary

Technical Problem

The existing synthesis method of 2-methoxy-4-amino-5-ethylsulfonylbenzoic acid has problems such as expensive reaction raw materials, hazardous solvents, cumbersome steps or low yield, making it difficult to meet the needs of industrial production and commercialization.

Method used

Using 2-methoxy-4-aminobenzoic acid methyl ester and acetic anhydride, concentrated sulfuric acid, phosphorus pentachloride, sodium sulfite, bromoethane and other compounds to carry out a series of reactions, after multi-step protection, purification and recrystallization, finally Obtain the target product.

Benefits of technology

It achieves efficient, safe and simplified operations, improves product yield and applicability for industrial production, and reduces process complexity and the use of hazardous substances.

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Abstract

The invention relates to a synthesis method for 2-methoxyl-4-amino-5-ethylsulfonylbenzoic acid which is an important immediate for antipsychotics Amisulpride. The method uses 2-methoxyl-4-methyl anthranilate as raw material, and carries out amino protection, sulphurization, deamination protection, chloridization, reduction, thylization, esterolysis and crystallization, and then the 2-methoxyl-4-amine-5-ethylsulfonylbenzoic acid is prepared. The method uses common reagents with easy obtainment as reaction mediums, the reaction condition is high, and the prepared product has the advantages of high purity and high yield, and is suitable for industrialization production.
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