Process for the preparation of candesartan cilexetil form i

A technology of candesartan cilexetil and sartan alkyl ester, which is applied in the field of preparation of candesartan cilexetil crystal form I, can solve the problem that small particles are sticky, easy to agglomerate, etc. question

Inactive Publication Date: 2009-08-26
新梅斯托克尔卡托瓦纳兹德拉韦尔公司
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  • Abstract
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  • Claims
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Problems solved by technology

On the other hand, such small particles have a tendency to stick and tend to agglom

Method used

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  • Process for the preparation of candesartan cilexetil form i
  • Process for the preparation of candesartan cilexetil form i
  • Process for the preparation of candesartan cilexetil form i

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Embodiment Construction

[0022] An object of the present invention is to prepare candesartan cilexetil crystalline form I with an average particle size below 25 μm and no tendency to agglomerate.

[0023] According to a first specific embodiment of the present invention, candesartan cilexetil is prepared by the following method, which method includes the following steps:

[0024] a) Esters of 1-((2'-cyano(1,1'-biphenyl)-4-yl)methyl)-2-ethoxy-1H-benzimidazole-7-carboxylate , preferably an alkyl ester thereof, converted into an ester, preferably a candesartan alkyl ester;

[0025] b) hydrolyzing the candesartan (alkyl) ester to obtain candesartan;

[0026] c) tritylating candesartan to obtain trityl candesartan;

[0027] d) esterification of trityl candesartan to obtain trityl candesartan cilexetil;

[0028] e) deprotecting trityl candesartan in the presence of Lewis acid to obtain candesartan cilexetil;

[0029] f) Crystallization of candesartan cilexetil from alcohol to obtain candesartan cilexeti...

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Abstract

The present invention provides an improved process for the manufacture of candesartan cilexetil form I. Further the present invention discloses a candesartan cilexetil preparation containing less than 0.15%, preferably less than 0.10%, of (+-)-1-Hydroxyethyl candesartan oxanyl carbonate (ester) of the following formula (V) wherein one of A, B and C is an oxygen atom and the other two are-CH2-groups.

Description

technical field [0001] The present invention relates to an improved process for the preparation of crystalline form I of candesartancilexetil having an average particle size below 25 μm and no tendency to agglomeration. Background technique [0002] Candesartan cilexetil, shown in formula (I) below, is chemically described as (+ / -)-1-[[(cyclohexyloxy)carbonyl]oxy]-2-ethoxy- 1-[[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate. Another representation is (+-)-1-hydroxyethyl-2-ethoxy-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)-7-benzimidazole -Carboxylate cyclohexyl carbonate, in which candesartan is the base carboxylic acid, ie 2-ethoxy-1-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)- 7-Benzimidazole carboxylic acid. [0003] [0004] Due to its ability to inhibit angiotensin-converting enzyme, candesartan cilexetil is widely used in the treatment of hypertension and related diseases and conditions. As an angiotensin II receptor antagonist, candesartan ...

Claims

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Application Information

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IPC IPC(8): C07D309/12C07D403/10C07D407/14A61K31/4184A61P9/00C07C22/00
Inventor 西尔沃·祖普契奇普里莫兹·贝恩基克波拉纳·斯姆尔科尔伊苏扎纳·塞尼卡尔尼韦斯·绍什塔里奇-维尔兹耶尔内伊·赫娃拉尼韦斯·绍什塔里奇－维尔兹
Owner 新梅斯托克尔卡托瓦纳兹德拉韦尔公司
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