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Preparation method of Olmesartan Medoxomil

A technology of olmesartan medoxomil and compounds, which is applied in the field of preparation of olmesartan medoxomil, can solve the problems of low yield, achieve high conversion rate, accelerate reaction speed, and facilitate industrialization

Active Publication Date: 2013-09-18
湖南欧亚药业有限公司
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Problems solved by technology

[0024] The synthesis of compound III all adopts methyl bromide, no matter use N-bromosuccinimide or dibromohydantoin as brominated reagent, all will The by-p

Method used

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  • Preparation method of Olmesartan Medoxomil
  • Preparation method of Olmesartan Medoxomil
  • Preparation method of Olmesartan Medoxomil

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[0056] In order to make the technical means, creative features, work flow, and use method of the present invention easy to understand and understand the purpose and effect of the present invention, the present invention will be further described with reference to specific embodiments.

[0057] Synthesis of compound 4:

[0058] Under the protection of nitrogen, add 31.2g of magnesium powder (1.30mol) and 5.6g of iodine (0.022mol) into the reaction flask, heat until the iodine vapor is full of the reaction flask, and then add 18.5g of p-chlorophenylglycol formal (compound 3 ) (0.10mol) and 50ml of tetrahydrofuran, then stir to reflux, then add 2.54g of iodine (0.01mol), 184.5g of p-chlorophenyl glycol formal (compound 3) (1.00mol), 200ml

[0059] Tetrahydrofuran and 200ml of toluene were reacted at reflux for 5 hours. The reaction solution was cooled to room temperature and allowed to stand under the protection of nitrogen to obtain a grid (1.00mol), 13.9g anhydrous manganese chlori...

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Abstract

The invention discloses a preparation method of Olmesartan Medoxomil. The method is used for synthesizing an important intermediate 4-[2-(2-triphenylmethyl tetrazole-5-yl) phenyl] benzyl bromide (a compound III) so as to prepare the compound Olmesartan Medoxomil. The method is high in yield, easy to separate and purify, simple to operate and suitable for industrial production.

Description

Technical field [0001] The present invention is a pharmaceutical chemical industry, and it involves a method to prepare Omesa. [0002] Background technique [0003] Olmesartan Medoxomil (compound Ⅰ) is an anterior drug, which is absorbed by the gastrointestinal tract after orally. Hydrolysis is a product of biological activity --- Omeartan and play a role., It can be taken for a long time.Omesa is a powerful and specific vascular tensionin II receptor antagonist, which selectively acts on AT 1 Receptor, prevent vascular tension Ⅱ and AT 1 The combination of receptors relax the smooth muscle of the blood vessels, which reduces blood pressure.Omeshadin was developed by Japan SANKYO and Forest Laboratories in the United States. It was listed in the United States in May 2002 and was listed in Germany in October of the same year. [0004] [0005] Ⅰ [0006] There are many synthesis research on Omeshadatt, mostly connected from pyramazole parts.It can be divided into two categories...

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Application Information

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IPC IPC(8): C07D405/14
Inventor 林开朝
Owner 湖南欧亚药业有限公司
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