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Hydrated perindopril salt, preparation method thereof and composition containing the same

A technology of perindopril and perindopril hydrate, which is applied in the field of perindopril hydrate salt, its preparation and use, and compositions containing it, and can solve the problems of time-consuming preparation methods and the like

Inactive Publication Date: 2007-05-23
CIPLA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Prior art methods for the preparation of perindopril or a pharmaceutically acceptable salt thereof generally tend to be time consuming and often result in unwanted related impurities such as diketopiperazine analogues

Method used

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  • Hydrated perindopril salt, preparation method thereof and composition containing the same
  • Hydrated perindopril salt, preparation method thereof and composition containing the same
  • Hydrated perindopril salt, preparation method thereof and composition containing the same

Examples

Experimental program
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Effect test

Embodiment 1

[0049] The (2S, 3aS, 7aS)-1-{2-[1-(ethoxycarbonyl)-(S)-butylamino]-(S)-propionyl}-octahydroindole-2-carboxylic acid The benzyl ester, perindopril benzyl (10 g) was dissolved in isopropanol (100 mL). To the clear solution was added tert-butylamine (2.5g) and 10% w / w palladium on charcoal (2g). at 1kg / cm 2 The reaction mixture was hydrogenated under pressure for 2 hours.

[0050] The reaction mass was filtered to remove the catalyst. Concentrate in vacuo to remove solvent and replace isopropanol by concurrent addition of ethyl acetate. The obtained solid was cooled to 0EC and filtered to obtain perindopril (7.8g).

Embodiment 2

[0052] Perindopril (10 g) was suspended in acetone (80 mL). Water (0.4 mL) was added thereto, and the contents were heated until the solids dissolved and cooled to room temperature. The resulting slurry was filtered to obtain perindopril monohydrate (9.4 g).

Embodiment 3

[0054] Perindopril (20 g) was suspended in ethyl acetate (300 mL). To this was added water (1.5 mL) and the contents were heated until the solids dissolved and cooled to 10EC. The resulting slurry was filtered to obtain perindopril monohydrate (17 g).

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Abstract

The present invention relates to a pharmaceutically acceptable salt of hydrated perindopril of formula (1a) wherein n is an integer of 1 to 5, or a reciprocal of integers 2 to 5. The present invention also relates to a process for preparing the salt, the use and the pharmaceutical composition containing the same.

Description

[0001] This application is a divisional application of the Chinese patent application 200380108700.2 filed on November 18, 2003, and the invention name is "perindopril". technical field [0002] The present invention relates to a process for the preparation of pharmaceutically acceptable salts of perindopril and their new polymorphs. Background technique [0003] The international non-proprietary trade name of perindopril is (2S, 3aS, 7aS)-1-{2-[1-(ethoxycarbonyl)-(S)-butylamino]-(S)-propionyl}- Octahydroindole-2-carboxylic acid. Perindopril is known to have therapeutic applications as an angiotensin converting enzyme (ACE) inhibitor. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to angiotensin II and causes the degradation of bradykinin. Angiotensin II is a vasoconstrictor that also stimulates aldosterone secretion through the adrenal cortex. Therefore, inhibition of ACE has demonstrated therapeutic application in patients suffering from di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/06A61K38/05A61P9/12A61P9/04A61P25/28A61K38/00A61P9/00
CPCC07K5/06026A61K38/00Y02P20/55A61P25/28A61P43/00A61P9/00A61P9/04A61P9/12Y02A50/30C07D209/42A61K31/404
Inventor 达尔迈拉杰·拉马钱德拉·拉奥拉金德拉·纳拉扬拉奥·坎坎
Owner CIPLA LTD
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