Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF8 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, such small particles have a tendency to stick and tend to agglomerate, which is highly undesirable in the preparation of pharmaceutical formulations

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

Examples

Experimental program
Comparison scheme
Effect test

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com