R-amisulpride medicine salt, preparation method, crystal form and application thereof

A kind of amisulpride medicine, the technology of amisulpride, which is applied in the field of preparation of R-amisulpride medicinal salt, can solve the problems such as the undeveloped R-amisulpride medicinal salt research, and achieve convenient scale The effect of chemical production, high safety and high optical purity
CN106995397AActive Publication Date: 2017-08-01SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
Publication Date
2017-08-01

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Abstract

The invention concretely relates to R-amisulpride medicine salt, a preparation method, a crystal form and application thereof in preparing a medicine for treating diabetes. The preparation method comprises the following steps: by adopting 2-aminomethyl-N-ethyl pyrrolidine as a raw material, and adopting L-tartaric acid, for splitting to obtain (R)-2-aminomethyl-N-ethyl pyrrolidine; directly condensing amisulpride acid and the (R)-2-aminomethyl-N-ethyl pyrrolidine under the catalysis of isopropyl chlorocarbonate and triethylamine, thus obtaining R-amisulpride; reacting the R-amisulpride obtained in the step (2) and acid to obtain the R-amisulpride medicine salt. The preparation method has the advantages of simplicity in operation, high safety, good product quality, low cost and the like, and is convenient for scale production.
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Description

technical field

[0001] The present invention relates to the field of medicine, in particular to R - Medicinal salt of amisulpride, preparation method, crystal form and use thereof. Background technique

[0002] Amisulpride, English name: Amisulpride, chemical name: 4-amino- N -[(1-Ethyl-2-pyrrolidinyl)methyl]-5-(ethylsulfonyl)-2-methoxybenzamide. It is a new type of non-classic antipsychotic drug developed by Sanofi-Synthelabo (Sanofi-Synthelabo) in France. Listed in China, the current domestic market demand is relatively wide, which has far-reaching economic and social significance. However, compared with traditional antipsychotic drugs, amisulpride has a low risk of inducing weight gain, diabetes and extrapyramidal side effects. At present, the clinical drug form of amisulpride is administered as a racemate.

[0003] research shows, S -Amisulpride is the active isomeric form of racemic amisulpride, which is twice as potent as the racemic form and is more potent than d...

Claims

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