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Sartan compound discoloration method

A technology of losartan and irbesartan, which is applied in the field of medicine and chemical industry, can solve the problems of many processes, material loss, three wastes and the like, and achieves the effects of simple operation, low cost and environmental friendliness

Inactive Publication Date: 2017-05-17
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above operations often produce a large amount of three wastes, resulting in material loss, more processes, and greater loss

Method used

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  • Sartan compound discoloration method
  • Sartan compound discoloration method

Examples

Experimental program
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Effect test

preparation example

[0022] Step 1: Add 200ml of toluene, 45g of biphenyl bromide, 30g of imidazole aldehyde, and 0.5g of tetrabutylammonium bromide in sequence; add aqueous sodium hydroxide solution and react at room temperature until the raw materials are completely reacted, separate layers, and wash. The organic layer was reduced by adding a reducing agent, crystallized by adding water, filtered, and dried to obtain the compound shown in Formula 1.

[0023] Second step: add 150ml of nitrogen methylpyrrolidone successively; 43g of compound shown in input formula (1), catalyzer, sodium azide 30g, react, reaction finishes, extract product with sodium hydroxide aqueous solution, add sodium nitrite, ethyl acetate Add hydrochloric acid dropwise until the pH reaches 3-5, filter, and wash the filter cake with water to obtain a yellow to brown crude wet product of losartan.

example 1

[0025] Add 50g of losartan obtained by the above route into the three-necked flask, add 150ml of water; dropwise add sodium hydroxide solution to dissolve it, add 1g of potassium borohydride at 20°C, stir for 3 hours, add a small amount of ethyl acetate, dropwise add hydrochloric acid to dissociate , to obtain off-white losartan (yield 98.5%, purity 99.0%). It can be used for the subsequent preparation of losartan potassium without decolorization.

example 2

[0027] Add 50g of losartan obtained by the above route into the three-necked flask, add 150ml of water; dropwise add sodium hydroxide solution to dissolve it, add 3g of potassium borohydride at 20°C, stir for 3 hours, add a small amount of ethyl acetate, dropwise add hydrochloric acid to dissociate , to obtain white losartan (yield 98.6%, purity 98.6%). It can be used for the subsequent preparation of losartan potassium without decolorization.

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Abstract

The invention relates to a sartan compound discoloration method. The method comprises the following steps: adding irbesartan or losartan crude products containing pigment impurities into solvent, and dissolving; and adding hydroboration reagent, stirring for discoloration, and crystallizing through dissociation, cooling, distillation and other means to obtain white losartan or irbesartan. The method has the advantages of mild reaction conditions, short operating cycle, high discoloration efficiency and environment friendliness, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to a method for removing color impurities of sartan compounds. [0002] technical background [0003] During the chemical synthesis process, due to side reactions, the material is unstable, and one or more color impurities are often produced. The color impurities generally account for a very low proportion of the material, and even general chromatography methods such as liquid chromatography and gas chromatography not detected. Color impurities will not have a great impact on the purity of the material, but it will have a greater impact on human senses. In order to remove the color in the drug, physical adsorption methods such as recrystallization, activated carbon, and diatomaceous earth are usually required for decolorization. However, many color impurities cannot be effectively removed by the above conventional methods. [0004] Losartan Potassium and Irbesartan are...

Claims

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Application Information

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IPC IPC(8): C07D403/10
CPCC07D403/10
Inventor 张霭文董鹏郑扬程龙沈波涛
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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