High-purified tropisetron hydrochloride compound

A technology of tropisetron hydrochloride and tropisetron, which is applied in the field of medicine, can solve the problems of low purity of finished products and affect the safety of pharmaceutical preparations, and achieve the effects of high yield, low cost and optimized product quality

Inactive Publication Date: 2010-07-28
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There are many synthetic methods of tropisetron hydrochloride reported in the literature, but there is a common defect that the purity of the finished product obtained is low, which affects the safety of pharmaceutical preparations

Method used

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  • High-purified tropisetron hydrochloride compound
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The refining of embodiment 1 tropisetron hydrochloride

[0018] (1) 50g tropisetron hydrochloride crude product is dissolved in 500ml water, then slowly add 10% (g / ml) sodium carbonate solution, stir and react until the solution pH is 8, produce tropisetron precipitation, filter, 50 ℃ Drying under reduced pressure gave 41.7 g of tropisetron.

[0019] (2) Dissolve 41.7 g of Tropisetron obtained in the previous step in 300 ml of n-butanol, add 3.5 g of activated carbon, stir at room temperature for 35 minutes, filter for decarburization, and collect the filtrate.

[0020] (3) The filtrate obtained in the previous step is separated and purified by a preparative chromatographic column to obtain creatine sodium phosphate refined product, wherein the mobile phase used in the chromatographic column is dichloromethane and volume accounting for 65% of mobile phase by volume Hydrochloric acid aqueous solution with a pH of 1; the stationary phase filler is silica gel; the flow ra...

Embodiment 2

[0027] The refining of embodiment 2 tropisetron hydrochloride

[0028] (1) 50g tropisetron hydrochloride crude product is dissolved in 500ml water, then slowly add the sodium hydroxide solution of 8% (g / ml), stirring reaction is 9 to solution pH, produces tropisetron precipitation, filters, 40 °C and dried under reduced pressure to obtain 41.3 g of tropisetron.

[0029] (2) Dissolve 41.3 g of Tropisetron obtained in the previous step in 300 ml of n-hexane, add 3.3 g of activated carbon, stir at room temperature for 45 minutes, filter for decarburization, and collect the filtrate.

[0030] (3) The filtrate obtained in the previous step is separated and purified by a preparative chromatographic column to obtain creatine sodium phosphate refined product, wherein the mobile phase used in the chromatographic column is dichloromethane whose volume accounts for 45% of the mobile phase and 55% dichloromethane whose volume accounts for the mobile phase Hydrochloric acid aqueous soluti...

Embodiment 3

[0037] The refining of embodiment 3 tropisetron hydrochloride

[0038] (1) 50g tropisetron hydrochloride crude product is dissolved in 500ml water, then slowly add the sodium bicarbonate solution of 12% (g / ml), stirring reaction is 7 to solution pH, produces tropisetron precipitation, filters, 40 °C and dried under reduced pressure to obtain 42.0 g of tropisetron.

[0039] (2) Dissolve 42.0 g of Tropisetron obtained in the previous step in 300 ml of n-hexane, add 3.2 g of activated carbon, stir at room temperature for 40 minutes, filter for decarburization, and collect the filtrate.

[0040] (3) The filtrate obtained in the previous step is separated and purified by a preparative chromatographic column to obtain creatine sodium phosphate refined product, wherein the mobile phase used in the chromatographic column is dichloromethane and volume accounting for 60% of mobile phase by volume Hydrochloric acid aqueous solution with a pH of 1; the stationary phase filler is silica g...

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Abstract

The invention relates to a tropisetron hydrochloride compound. The purity of the tropisetron hydrochloride is greatly improved by acid-base reaction, activated carbon adsorption and separation and purification prepared chromatographic columns, thus optimizing the quality of preparation products and the safety of clinical medication. The method has simple process, low cost and high yield, and is applicable to industrial production.

Description

technical field [0001] The invention relates to a tropisetron hydrochloride compound, which can obtain high-purity tropisetron hydrochloride through the method of the invention, and belongs to the technical field of medicine. Background technique [0002] Tropisetron hydrochloride, its chemical name is: endo-1H-indole-3-carboxylic acid-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester hydrochloride, molecular formula: C 17 h 20 N 2 o 2 HCl, molecular weight: 320.81, structural formula: [0003] [0004] Tropisetron hydrochloride is a potent and highly selective competitive antagonist of peripheral neurons and central nervous system 5-hydroxytryptamine 3 (5-HT3) receptors, mainly by selectively blocking the presynaptic 5-HT3 receptors inhibit the gag reflex. It is indicated for the prevention and treatment of nausea and vomiting induced by cancer chemotherapy. [0005] There are many synthetic methods of tropisetron hydrochloride reported in the literature, but there is a ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D451/12
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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