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Impurity removal method of rosiglitazone hydrochloride

A technology of rosiglitazone hydrochloride and crude product, applied in the field of pharmaceutical synthesis, can solve the problems of impurity I being difficult to consume, unable to completely remove impurities and cost input, and achieve the effects of low cost, mild conditions and simple operation

Pending Publication Date: 2021-06-25
RUYUAN HEC PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to overcome the defects and deficiencies that impurity I is difficult to completely consume in the production of existing rosiglitazone hydrochloride, and cannot be completely removed by repeated refining and high cost investment, and provide a premise of ensuring the yield Next, the impurity removal method of the rosiglitazone hydrochloride that significantly reduces impurity I

Method used

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  • Impurity removal method of rosiglitazone hydrochloride
  • Impurity removal method of rosiglitazone hydrochloride
  • Impurity removal method of rosiglitazone hydrochloride

Examples

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Effect test

Embodiment 1

[0026] Embodiment 1 A kind of method for removing impurities of rosiglitazone hydrochloride

[0027] The impurity-removing method of described rosiglitazone hydrochloride comprises the following steps:

[0028] Add 10 g of crude rosiglitazone hydrochloride (the content of impurity I is 0.7%), add 70 g of methanol, heat to 55 ° C to dissolve and clarify, then slowly add 0.1 g of magnesium powder for reaction, stir for 15 min, filter, and adjust the pH of the filtrate with hydrochloric acid when the filtrate is heated = 2 to 3, stirred for 30 minutes, then cooled the filtrate until a large amount of solids were precipitated, stirred at 0°C for 1 hour, filtered, rinsed, and dried to obtain high-purity rosiglitazone hydrochloride with a yield of 90% and an impurity I content of <0.01% or disappear.

Embodiment 2

[0029] The influence of embodiment 2 different solvents, ratio on the effect of removing impurities of rosiglitazone hydrochloride

[0030] With reference to the impurity removal method in Example 1, change the ratio of methanol or crude rosiglitazone hydrochloride to methanol, and remove impurities from the crude product of rosiglitazone hydrochloride (the content of impurity I is 0.7%). The effect of impurity removal is shown in Table 1 .

[0031] Table 1 The effect of different solvents and ratios on the removal of impurities of rosiglitazone hydrochloride

[0032] serial number solvent Crude product: solvent Impurity I content after impurity removal (%) Yield (%) 1 (Example 1) Methanol 1:7 <0.01

[0033] As can be seen from Table 1, after using methanol as solvent and the crude product of rosiglitazone hydrochloride to remove impurities according to a certain ratio, the content of impurity I is significantly reduced, and even can be completely rem...

Embodiment 3

[0034] The influence of embodiment 3 different reducing agents on the effect of removing impurities of rosiglitazone hydrochloride

[0035] With reference to the impurity removal method in Example 1, the reducing agent was changed to remove impurities from the crude product of rosiglitazone hydrochloride (the content of impurity I was 0.7%). See Table 2 for the effect of impurity removal.

[0036] Table 2 The impurity removal effect of different reducing agents and addition amounts on rosiglitazone hydrochloride

[0037]

[0038]

[0039] As can be seen from Table 2, after using different reducing agents and the crude product of rosiglitazone hydrochloride to remove impurities according to a certain ratio, the content of impurity I is significantly reduced, and even can be completely removed, and the effect of removing impurities is very good; but when the reducing agent is boron During potassium hydride or sodium borohydride, although impurities can also be removed, the...

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Abstract

The invention belongs to the technical field of medicine synthesis, and particularly relates to an impurity removal method of rosiglitazone hydrochloride. According to the method, a reducing agent is added into a rosiglitazone hydrochloride crude product and can react with residual hydrogen ions in the crude product, hydrogen atoms with high reducibility are generated and react with an impurity I, the impurity I can be consumed to a great extent and even completely consumed, and the effect of remarkably reducing the impurity I can be achieved without repeated impurity removal; meanwhile, relatively high yield can be kept; and the impurity removal method is simple to operate, mild in condition, low in cost and suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis. More specifically, it relates to a method for removing impurities of rosiglitazone hydrochloride. Background technique [0002] Rosiglitazone (rosiglitazone) is a thiazolidinedione hypoglycemic drug, which can reduce blood sugar by increasing the sensitivity of tissues to insulin and improving the utilization of glucose by cells, and can significantly reduce fasting blood sugar, insulin and C-peptide. It can also significantly reduce postprandial blood sugar and insulin, and significantly reduce the level of glycosylated hemoglobin (HbAlc). [0003] Rosiglitazone is often made into rosiglitazone hydrochloride tablets for oral administration, but it is found in actual production and application that during the synthesis of rosiglitazone or rosiglitazone hydrochloride, there is a raw material impurity I: 5-(4-( (2-(N-methyl-N-(2-pyridyl)amino)ethoxy)phenyl)methylene)-2,4-thiazolidinedi...

Claims

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Application Information

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IPC IPC(8): C07D417/12
CPCC07D417/12
Inventor 徐形典林德樟张志勇贺江华葛玉聪
Owner RUYUAN HEC PHARM
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