Synthetic method of 2-methoxyl-4-amino-5-ethyl sulfuryl methyl benzoate

Abstract

The invention relates to a synthetic method of 2-methoxyl-4-amino-5-ethyl sulfuryl methyl benzoate. The synthetic method comprises the following steps: carrying out halogenation (chlorination, bromination and iodization) pm 2-methoxyl-4-acetamido methyl benzoate by halogens; and then, condensing the halogenated 2-methoxyl-4-acetamido methyl benzoate with ethyl sodium sulfinate to obtain a target product. The synthetic method has the advantages of simple process line, high product yield (the total yield reaches 80%) and good product quality (the purity reaches 99.5%), and the 2-methoxyl-4-amino-5-ethyl sulfuryl methyl benzoate is white in appearance.

Description

technical field

[0001] The invention relates to the technical field of preparation of pharmaceutical intermediates, in particular to a synthesis method of methyl 2-methoxy-4-amino-5-ethylsulfone benzoate. 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 product through deacetylation, th...

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