Method for preparing 2-methoxy-4-amino-5-ethysulfonyl benzoic acid methyl ester by halogen halogenation

Abstract

The invention relates to a method for preparing 2-methoxy-4-amino-5-ethysulfonyl benzoic acid methyl ester by halogen halogenation. According to the invention, 2-methoxy-4-acetyl methyl anthranilate is subjected to halogen halogenation (chlorination, bromination or iodization) and then is condensed with sodium ethanesulfinate to obtain a target product. The method has the advantages that the process route is simple, the product yield is high, the total yield reaches 80 percent, the product quality is high, the purity reaches 99.5 percent, and the appearance is white.

Description

technical field

[0001] The invention relates to the technical field of preparation of pharmaceutical intermediates, in particular to a method for preparing methyl 2-methoxy-4-amino-5-ethylsulfonylbenzoate by halogenation with halogen. Background technique

[0002] Psychosis refers to a serious psychological disorder, in which there may be persistent and obvious abnormalities in the mental activities of patients such as cognition, emotion, will, action and behavior; they cannot study, work, and live normally; their actions and behaviors are difficult to be understood by ordinary people; Under the control of morbid psychology, there are actions of suicide or attacking or hurting others. 2-methoxy-4-amino-5-ethylsulfonylbenzoic acid is an important intermediate of the antipsychotic drug amisulpride. There are many related reports on its synthetic route, and the main routes used in industrial production are as follows:

[0003]

[0004] The route is to obtain the target pro...

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