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Refining method of olmesartan medoxomil

A technology of olmesartan medoxomil and a purification method, which is applied in the field of drug synthesis and achieves the effects of stable process, high product purity and simple process

Inactive Publication Date: 2018-02-06
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most industrial research and application is the first method. After exhaustive literature search, we found that most of the literature is about the synthesis route of olmesartan medoxomil, and there are few reports about the refining method of olmesartan medoxomil

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Put 20g of crude olmesartan medoxomil and 600ml of dichloromethane into the reaction flask, raise the temperature to 40°C, all the solids are dissolved, add 0.5g of activated carbon, reflux for 20min, keep warm at 40°C and filter, and collect the filtrate. Reheat the filtrate to reflux, stop heating and cool down to 0°C, stir and crystallize for 12 hours, filter, wash the filter cake with 50ml of n-hexane, and vacuum dry at 40°C for 12 hours to obtain 18.0g of fine olmesartan medoxomil.

Embodiment 2

[0025] Put 20g of crude olmesartan medoxomil and 640ml of dichloromethane into the reaction flask, raise the temperature to 42°C, all the solids are dissolved, add 0.5g of activated carbon, reflux for 30min, heat-preserve and filter, and collect the filtrate. Reheat the filtrate to reflux, stop heating and cool down to 0°C, stir and crystallize for 12 hours, filter, wash the filter cake with 50ml of n-hexane, and vacuum dry at 60°C for 12 hours to obtain 17.1g of fine olmesartan medoxomil.

Embodiment 3

[0027] Put 20g of crude olmesartan medoxomil and 580ml of chloroform into the reaction flask, raise the temperature to 40°C, all the solids are dissolved, add 0.5g of activated carbon, reflux for 1h, keep warm at 40°C and filter, and collect the filtrate. Reheat the filtrate to reflux, stop heating and cool down to 0°C, stir and crystallize for 12 hours, filter, wash the filter cake with 50ml of n-heptane, and vacuum dry at 40°C for 12 hours to obtain 17.3g of fine olmesartan medoxomil.

[0028] Table 1 Olmesartan Medoxomil Refining Effect Data Comparison

[0029] Refining method

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PUM

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Abstract

The invention belongs to the field of drug synthesis and relates to a refining method of high-purity olmesartan medoxomil. The refining method of olmesartan medoxomil comprises the steps as follows: acrude olmesartan medoxomil product is added to an organic solvent, heated and stirred to be completely dissolved, activated carbon decoloration is performed, natural cooling for crystallization is performed, filtration and drying are performed, and the high-purity olmesartan medoxomil is obtained. With the adoption of the method, the product purity is 9.5% or above and the refinement yield is notlower than 85%. Besides, the refining method comprises a simple and stable process, is convenient to operate, low in production cost and suitable for industrial production, and the product purity ishigh.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a method for refining olmesartan medoxomil. Background technique [0002] Olmesartan medoxomil is an angiotensin II receptor antagonist. After oral administration, it is absorbed through the gastrointestinal tract and hydrolyzed into a biologically active product——Olmesartan. It is the seventh drug approved by the US FDA for the treatment of hypertension. Angiotensin II receptor antagonist, which was successfully developed by Japan Sankyo Corporation in 1991, has good curative effect on various types of hypertension, and its outstanding features are long half-life, small dosage, and quick onset. [0003] A lot of research has been done on the synthesis method of olmesartan medoxomil at home and abroad. US5616599 disclosed two kinds of synthesis methods of olmesartan medoxomil at the earliest. The first method is: the biphenyl part is connected with the imidazole part and then hydr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/14
CPCC07D405/14
Inventor 严洁王志凤
Owner TIANJIN HANKANG PHARMA BIOTECH