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Preparation method for high-purity sulpiride or optical isomers thereof

An optical isomer, high-purity technology, applied in the field of medicine, can solve the problems of large dosage, high production cost, low solubility, etc., and achieve the effects of reducing the amount of related substances, reducing production costs, and reducing the material feeding ratio.

Active Publication Date: 2014-05-07
JIANGSU TASLY DIYI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, due to the low solubility of sulpiride and levosulpiride in ethanol, the use of 95% ethanol to refine the solvent requires a large amount, and the feed ratio is above 1:10, the production cost is high, and the yield is only about 85-90%.

Method used

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  • Preparation method for high-purity sulpiride or optical isomers thereof
  • Preparation method for high-purity sulpiride or optical isomers thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Add 160g of 90% ethanol to the reaction flask, add 20g of the crude product of sulpiride, heat and stir under the protection of nitrogen until the crude product is completely dissolved, cool slightly, add 0.8g of activated carbon, stir under reflux for 5 minutes, filter while it is hot, and cool the filtrate to 0-5 Stir at ℃ for 1 hour, filter, wash with 90% ethanol, and dry at 70℃ for 2 hours. The product was obtained with a yield of 90.3%. Related substances are less than 0.15%.

Embodiment 2

[0042] Add 100g of 70% ethanol to the reaction flask, add 20g of the crude product of sulpiride, under the protection of nitrogen, heat and stir until the crude product is completely dissolved, filter while it is hot, cool the filtrate to 0-5°C and stir for 0.5 hours, filter, wash with 70% ethanol, Dry at 70°C for 2 hours. The product was obtained with a yield of 95.4%. Related substances are less than 0.1%.

Embodiment 3

[0044] Add 70g of 40% ethanol to the reaction flask, add 10g of crude sulpiride, heat and stir until the crude product is completely dissolved, cool slightly, add 0.1g of activated carbon, stir at reflux for 15 minutes, filter while it is hot, cool the filtrate to 0-5°C and stir for 1 hour , filtered, washed with 40% ethanol, and dried at 70°C for 2 hours. The product was obtained with a yield of 92.2%. Related substances are less than 0.1%.

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Abstract

The invention relates to a preparation method for high-purity sulpiride or optical isomers thereof. The method comprises the following steps: first, crude products of sulpiride or optical isomers thereof are added in ethanol aqueous solutions with different concentrations of 10-90%, under a normal condition or under protection of inert gases (nitrogen usually), the solutions are heated and the crude products are dissolved, when the solutions are cooled slightly, active carbon is added for decolouring or is not added; second, filtration is carried out, the filtrate is cooled, crystals are precipitated, filtration, washing and drying are carried out. The charging ratio is small, ethanol dosage is decreased obviously, the refining efficiency is raised greatly, the production cost is lowered, the yield is raised, the impurity amount is decreased obviously and the product quality is raised greatly.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for preparing high-purity sulpiride or its optical isomers. Background technique [0002] Sulpiride, chemically named N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-(aminosulfonyl)benzamide, is a class of highly active Dopamine D2 receptor blocker. Synthesized by the French in 1967, and then listed in many countries around the world. Sulpiride has the effect of antidepressant and treatment of mental disorders, because of its strong antipsychotic effect and few adverse reactions, it has been used clinically for many years at home and abroad. [0003] Levosulpiride, chemical name (-)-(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-(aminosulfonyl)benzene Formamide is an optical isomer of sulpiride. Levosulpiride has anti-emetic and gastroparesis effects in addition to anti-depression and treatment of mental disorders. This single isomer compound was more potent and better tol...

Claims

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Application Information

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IPC IPC(8): C07D207/09
CPCC07D207/09
Inventor 刘文峥王国成刘金平
Owner JIANGSU TASLY DIYI PHARMA CO LTD
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