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Preparation method of olmesartan ester

A technology of olmesartan medoxomil and ethyl acetate, which is applied in the field of pharmaceutical synthesis, can solve the problems of harsh reaction conditions, low product purity and low yield, and achieves the effects of simple preparation process, high product purity and high yield

Inactive Publication Date: 2013-04-17
ANHUI YOUCARE KAIYUE PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The preparation process of olmesartan medoxomil in the prior art has many synthetic routes, and there are many defects such as low yield, harsh reaction conditions, and low product purity.

Method used

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  • Preparation method of olmesartan ester
  • Preparation method of olmesartan ester
  • Preparation method of olmesartan ester

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Embodiment Construction

[0025] Below in conjunction with embodiment and attached figure 1 The present invention is further described.

[0026] Add 4000ml of dioxane and 2708g (0.38mol) of the compound of formula (I) into a 10L three-necked flask, stir, cool in an ice-water bath to 10-15°C, and dropwise add a mixed solution of 244g (0.58mol) lithium hydroxide / 1425ml of water . After the dropwise addition, keep at 5-10°C for 10-12 hours. Concentrate under reduced pressure to the remaining 900ml of the reaction solution, add 4000ml ethyl acetate to the concentrated solution, and after fully stirring, separate the organic phase, dry the organic phase with anhydrous magnesium sulfate, filter, and concentrate to obtain a light yellow residue, i.e. formula (II ) compounds.

[0027] Add the light yellow residue (compound of formula (II)) into a 3000ml three-necked flask, add 1450ml N,N-dimethylaniline and 542g (0.39mol) of potassium carbonate in the there-necked flask, and add 903g (0.61mol) of potassium ...

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Abstract

The invention relates to the technical field of drug synthesis, in particular to a preparation method of olmesartan ester. The method comprises the following steps: adding 3950-4050ml of dioxane and 2700-2710 g of formula (I) compound into a reaction vessel, stirring, and cooling to 10-15 DEG C with an ice-water bath; and dropwise adding a mixed solution of 240-250g of lithium hydroxide and 1400-1450ml of water, and keeping 5-10 DEC C and reacting for 10-12 hours after dropwise adding. The preparation method of olmesartan ester has the advantages of simple preparation process and higher yield, is suitable for industrial production, and effectively shortens the reaction time. Meanwhile, the purification process is simpler, and the product purity is higher.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a preparation method of olmesartan medoxomil. Background technique [0002] Olmesartan medoxomil (Olmesartan Medoxomi I) was developed by Sankyo of Japan and Forest Laboratories of the United States. It was launched in the United States under the trade name Benicar in May 2002. It was approved in Germany in August of the same year and launched in early October. [0003] The curative effect of olmesartan is better than that of losartan and other earlier marketed sartan drugs. It is an ideal antihypertensive drug and has good curative effect on various types of high blood pressure. Its outstanding feature is its long half-life, which can be used in It can effectively control blood pressure within a day, so it is more convenient to take. At the same time, compared with other angiotensin receptor antagonist drugs, it has obvious advantages such as small dose, quick onset, str...

Claims

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Application Information

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IPC IPC(8): C07D405/14
Inventor 周如国
Owner ANHUI YOUCARE KAIYUE PHARMA