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

Preparation methods of losartan potassium and preparation thereof

A technology of losartan potassium and losartan, applied in the field of chemical pharmacy, can solve problems such as high production cost and complicated subsequent procedures, and achieve the effect of high yield

Active Publication Date: 2014-04-09
YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD +2
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of this process requires an N-alkylation catalyst with a relatively high market price, and the subsequent process is relatively complicated, and the production cost is relatively high

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
  • Preparation methods of losartan potassium and preparation thereof
  • Preparation methods of losartan potassium and preparation thereof
  • Preparation methods of losartan potassium and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0012] Below, in conjunction with embodiment the content of the present invention is described in detail.

[0013] 1, the preparation of raw material losartan potassium

[0014] Detailed steps

[0015] ①2-Butyl-4-chloro-5-(hydroxymethyl)-1-[[2'-[(triphenylmethyl)-tetrazolium-5-]biphenyl-4-]methyl] Imidazole (trityl losartan)

[0016] Main feeding ratio:

[0017] 2-Butyl-5(4)-formyl 186.5g (FW: 186.5) 1.0mol-4(5)-chloroimidazole(II)

[0018] N-(triphenylmethyl)-5-[(4'-557.0g (FW:557) 1.0mol bromomethyl)-biphenyl-2-]tetraazol

[0019] Azole(III)

[0020] Tetrabutylammonium bromide 32.2g (FW: 322) 0.1mol

[0021] Sodium hydroxide 80.0g (FW: 40) 2.0mol

[0022] Sodium borohydride 38.0g (FW: 38) 1.0mol

[0023] 2-Butyl-5(4)-formyl-4(5)-chloroimidazole (II) 186.5g (1.0mol), tetrabutylammonium bromide 32.2g (0.1mol), 1.0mol / L hydroxide Mix 2000ml (2.0mol) of sodium with 2.0L of dichloromethane, and add N-(triphenylmethyl)-5-[(4'-bromomethyl)-biphenyl-2-]tetrazolium ( III) ...

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

PropertyMeasurementUnit
melting pointaaaaaaaaaa
angle of reposeaaaaaaaaaa
Login to View More

Abstract

The invention discloses preparation methods of losartan potassium and a preparation thereof. The losartan potassium is prepared by the steps of: by taking 2-butyl-5(4)-formoxyl-4(5)-trichlorophenidin (II) and N-(triphenylmethyl)-5-[(4'-brooethyl)-xenyl-2-]tetrazole (III) as raw materials and adopting tetrabutyl ammonium bromide as a phase-transfer catalyst for N-alkylating, performing condensation, reduction and deprotection to synthesize losartan; and salifying the obtained losartan with potassium hydroxide to synthesize raw material losartan potassium. The raw material losartan potassium is mixed with proper auxiliaries to prepare a medicinal preparation. The preparation methods in the invention have the characteristics of mild requirements on production conditions, simplicity in operation and high yield, and are suitable for industrial production.

Description

technical field [0001] The invention relates to the field of chemical pharmacy. Especially the synthesis process of losartan potassium, sartan potassium hydrate, new crystal form IV losartan potassium and its solvate, new crystal form V losartan potassium and its solvate; the preparation of the compound Methods; compositions containing said compounds and uses of said compounds in medicine. Background technique [0002] In 1995, losartan potassium became the first non-peptide AT antagonist approved by the US Food and Drug Administration for clinical use. In particular, Falsartan is approved for the treatment of high blood pressure alone or in combination with other antihypertensive drugs. Falsartan can be administered orally as its potassium salt. Fusartan potassium tablets (Coz, aar.: Merck) containing the only active ingredient and compound fusartan potassium tablets (Hyzaar.: Merck) containing hydrogen acetaminophen are available by prescription. [0003] Falsartan pot...

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
Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/10B01J31/02
CPCY02P20/55
Inventor 李元波蓝海沙雪梅廖建
Owner YANGTZE RIVER PHARM GRP SICHUAN HAIRONG PHARM CO LTD
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