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Refining method of valsartan

A refining method and valsartan technology, applied in the field of medicinal chemistry, can solve the problems of increasing solvent residues, weak adsorption, low valsartan yield and the like

Inactive Publication Date: 2018-05-18
HUNAN QIANJIN XIELI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because valsartan is prone to hydrolysis under alkaline conditions, the patent No. CN 104402838 A discloses a method for refining valsartan using acidic or neutral alumina to adsorb impurities, but this method adsorbs some positively charged impurities The effect is not strong
The patent Nos. CN 103435567 A and CN 102391200 A all disclose the refining method of valsartan. Although these two methods can achieve the refining effect, the yield of valsartan after refining is low, and two solvents are used in the process or two or more solvents, increasing solvent residue

Method used

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  • Refining method of valsartan
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  • Refining method of valsartan

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Embodiment 1

[0064] Take about 80g of valsartan and 480mL of ethyl acetate, put them in the same 1000mL reactor, heat to dissolve, cool to room temperature, add 3.2g of activated carbon, and reflux at 80°C for 30 minutes for decolorization. Filtrate while it is hot, stir the filtrate mechanically at a speed of 200-300r / min, cool down naturally to about 15°C, crystallize overnight (about 16 hours), centrifuge, take another small amount of ethyl acetate to rinse the filter residue, centrifuge, put the filter residue Put it into a vacuum desiccator, dry at 50°C for about 2 hours, refine three batches continuously, and take it out to obtain the refined valsartan raw material.

[0065] Table 8 Comparison of valsartan purity and yield before and after refining

[0066]

[0067] As can be seen from the above table 8, the valsartan obtained by the refining process of the present invention has high purity (>99.5%), less impurities and high yield (>90%). And the three batches of continuous refin...

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Abstract

The invention discloses a refining method of valsartan. The refining method comprises two steps as follows: step 1, a crude valsartan product and ethyl acetate are placed in the same reactor and heated for dissolution, then, the obtained mixture is cooled to the room temperature, and activated carbon is added for reflux decolorization; step 2, the mixture is filtered while hot, a filtrate is naturally cooled, stirring crystallization is performed, centrifugation is performed after crystallization, a small amount of ethyl acetate is taken to elute solids, centrifugation is performed, a precipitate obtained after centrifugation is placed in a vacuum dryer and then taken out, and a refined valsartan material is obtained. The content of impurities in valsartan can be effectively reduced and the product purity (higher than 99.9) can be increased with the refining method. The refining method is simple to operate and suitable for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a method for refining valsartan. Background technique [0002] Valsartan is a new generation of angiotensin II receptor antagonist, which has high selectivity and special direct action, can effectively antagonize AT1 receptor, its half-life is about 9 hours, and its antihypertensive effect can be maintained for more than 24 hours, and has Better valley-to-peak ratio, with a wide range of therapeutic effects, and good patient tolerance. [0003] Because valsartan is a medicine for chronic diseases, it needs to be taken for a long time, so in order to prevent the side effects caused by the accumulation of impurities in the patient's body, it is urgent to develop a refining method for valsartan to ensure the purity of the product. [0004] Because valsartan is prone to hydrolysis under alkaline conditions, the patent No. CN 104402838 A discloses a method for...

Claims

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Application Information

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IPC IPC(8): C07D257/04
CPCC07D257/04
Inventor 谭喜平徐彬滨任超张泽昀
Owner HUNAN QIANJIN XIELI PHARMA CO LTD