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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

Active Publication Date: 2017-08-01
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few studies on R-amisulpride, and the research on R-amisulpride medicinal salt has not been carried out in the prior art

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 R -2-Aminomethyl- N -Ethylpyrrolidine- L - Synthesis of tartrate

[0060] Will L -Add 45.6 g of tartaric acid into 60 mL of distilled water, stir until it is completely dissolved, slowly add 30 g of 2-aminomethyl-N-ethylpyrrolidine dropwise, keep the temperature between 25°C and 30°C during the dropwise addition, After the addition, stir at room temperature for 1 h, then add 260 ml of methanol to the reaction flask, stir at 12±2°C for 2 h, filter, and wash the filter cake once with 20 ml of methanol. Filter, add the filter cake to 190 ml of 75% methanol, heat until clarified, naturally cool down to 20±2°C, stir for 1 h, filter with suction, rinse with 15 ml of methanol, and dry to obtain a colorless solid.

[0061] Will R -2-Aminomethyl- N -Ethylpyrrolidine- L -Dissolve 11 g of tartrate in 60 ml of distilled water, add 36 g of 30% sodium hydroxide solution dropwise, stir at 20±2°C for 1 h, extract with dichloromethane (30 ml×3), and combine The organic...

Embodiment 2

[0062] Example 2 R - Synthesis of amisulpride

[0063] Dissolve 10 g of amimic acid and 4.96 g of triethylamine in 50 ml of acetone, cool down to 5°C, slowly add 5.6 g of isopropyl chloroformate dropwise, after the dropwise completion, keep stirring for 0.5 h, then slowly add in Example 1 Prepared R -2-Aminomethyl- N - 25 mL of acetone solution of 6.42 g of ethylpyrrolidine, after dropping, stir at 12°C for 0.5 h, then move to room temperature and stir for 1 h. After rotary evaporation, water was added and extracted with dichloromethane (25 ml×3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and rotary evaporated to dryness to obtain a yellow-brown oil.

Embodiment 3

[0064] Example 3 R -Synthesis of amisulpride maleic acid

[0065] Prepared by Example 2 R - 10 g of amisulpride and 35 ml of methanol, heat to dissolve, add 4.06 g of maleic acid in methanol solution 15 ml, stir at 45°C for 5h, cool down to 3°C and stir for 3h, a large amount of crystals are precipitated, suction filtered, and dried , That is, 10.9g of the product was obtained with a yield of 83% and an optical purity of ee%=100%.

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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.

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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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/09A61K31/40A61P3/10
CPCC07B2200/13C07D207/09
Inventor 张恺薛娜石晓伟王磊吴玉鹏田欣柴仪
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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