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Lubiprostone refining method

A technology of lubiprostone and organic solvents, which is applied in the field of refined lubiprostone, can solve the problems of reducing production costs, and achieve the effects of simple operation, stable properties and reduced production costs

Inactive Publication Date: 2017-12-15
BEIJING SHENLANHAI BIO PHARM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on the research and reports that there is no suitable industrial production of high-purity lubiprostone in this field, we provide a method for refining lubiprostone here, which can not only obtain lubiprostone with higher purity, but also can be extremely Greatly simplify operations and reduce production costs

Method used

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Effect test

Embodiment 1

[0014] Put crude lubiprostone (100g) in isopropyl acetate (200mL), stir at 20-30°C to dissolve it. After dissolving, add activated carbon (5g) and stir at 20-30°C for 30 minutes. After stirring, filter out the activated carbon and rinse the filter cake with isopropyl acetate (50mL). Slowly add octane to the filtrate, crystallize at 15~25°C for 4 hours, filter with suction, and wash the filter cake with octane (200mL). The filter cake was vacuum-dried for 4 hours to obtain 95.3 g of off-white crystalline powder with a yield of 95.3% and a purity of 99.67%.

Embodiment 2

[0016] Put crude lubiprostone (10g) in acetone (35mL), stir at 20-30°C to dissolve it. After dissolution, tert-butyl methyl ether (100 mL) was slowly added. After the addition, keep stirring for 8 hours. After suction filtration, the filter cake was rinsed with methyl tert-butyl ether (20 mL), and dried at 25-35°C for 4 hours to obtain 7.95 g of off-white crystalline powder with a yield of 79.5% and a purity of 99.23.

Embodiment 3

[0018] The crude lubiprostone (50g) was placed in ethyl acetate (100mL), stirred at 20-30°C to dissolve it. After dissolving, add activated carbon (5g), stir at 20-30°C for 30 minutes, filter the activated carbon, and rinse the filter cake with ethyl acetate (10mL). Isooctane (1320 mL) was slowly added to the filtrate, and after the addition was completed, it was incubated and crystallized for 2 hours. Suction filtration, rinse the filter cake with isooctane (100mL), and dry at 25-35°C for 6 hours to obtain 43.2% off-white crystalline powder with a yield of 86.4% and a purity of 99.02%.

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Abstract

The invention relates to the field of pharmaceutical chemistry and provides a lubiprostone refining method. In comparison with existing lubiprostone preparation methods, the preparation method of the invention can be adopted to obtain high-purity lubiprostone more simply and with high yield through a recrystallization mode.

Description

technical field [0001] The invention provides a method for refining Lubiprostone. In the method, the crude lubiprostone is recrystallized in an organic solvent and crystallized at 20-30° C., so that the lubiprostone with a purity of not less than 99.0% can be obtained in a high yield. Background technique [0002] Lubiprostone, chemical name (2R,4aR,5R,7aR)-2-(1,1-difluoropentyl)-2-hydroxy-6-oxo-3,4,4a,5 ,7,7a-hexahydrocyclopenta[b]pyran-5-heptanoic acid, the chemical structure of which is: [0003] . [0004] Lubiprostone is the active pharmaceutical ingredient of the drug Amitiza® developed by Sucamp Company of the United States. Lubiprostone belongs to a chloride ion channel activator, which can specifically act on the type II chloride ion channel on the epidermal cell membrane of the gastrointestinal tract, stimulate the secretion of intestinal fluid with high chloride ion concentration, increase intestinal motility, and promote Softened stool passes through the bo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/94
CPCC07D311/94
Inventor 何杰张翔
Owner BEIJING SHENLANHAI BIO PHARM TECH
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