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Ozagrel ester, composition and production method thereof

A technology of ozagrel ester and its composition, which is applied in the field of ozagrel ester and its composition and preparation, and can solve the problems of ozagrel ester instability and curative effect reduction, etc.

Inactive Publication Date: 2008-07-16
王立峰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, ozagrel sodium injection dosage forms are mostly used clinically, but according to literature reports, ozagrel is unstable in aqueous solution and can be partially isomerized and converted into cis-imidazole methyl cinnamic acid, which reduces its curative effect

Method used

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  • Ozagrel ester, composition and production method thereof
  • Ozagrel ester, composition and production method thereof
  • Ozagrel ester, composition and production method thereof

Examples

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[0040] These pharmaceutical compositions can be prepared by mixing with suitable pharmaceutical additives such as excipients, disintegrants, binders, lubricants, diluents, buffers or by diluting and dissolving in suitable additives , isotonic agent, preservative, wetting agent, emulsifier, dispersant, stabilizer, solubilizer, etc., and prepare the pharmaceutical composition according to conventional methods.

[0041] When the pharmaceutical composition of the present invention is used for actual treatment, the dose of the compound represented by the above general formula as the active ingredient can be appropriately determined according to the age, sex, body weight, symptoms and degree of treatment of each patient. The dose is approximately 0.1-1,000 mg per adult per day, and the dose is approximately 0.01-500 mg per adult per day for parenteral administration, and the daily dose can be divided into one or several times a day and administered at an appropriate time .

[0042]...

Embodiment 1

[0049] [Example 1] (R, S)-1-(isopropoxycarbonyloxy)-ethyl-(Z)-3[4-(1H-imidazolyl-1-methyl)phenyl]-2- Preparation of Acrylates.

[0050]Put 22.8g of ozagrel into 120ml of DMA, add 2.7g of sodium acetate and 10ml of water under stirring, stir at 10-15°C for 30 minutes, cool to -5°C, add 27.2g of 1-iodoisopropoxycarbonyloxyethane , react at 0-5°C for 2.5 hours, pour into 200ml ethyl acetate, add 100ml 5% sodium bicarbonate solution, stir, separate the organic phase, extract the aqueous phase with 20ml ethyl acetate, combine ethyl acetate, no Dry over magnesium sulfate, filter, and evaporate the solvent under reduced pressure to obtain 52.3 g of white to off-white powder (yield 85%).

[0051] 1 H-NMR (CD 3 Cl, δ) 1.32(d, 6H), 1.76(d, 3H), 4.31(6-fold, 1H), 4.98(s, 2H), 6.40(d, 1H), 6.62(4-fold, 1H), 6.98-7.20(m, 6H), 7.62(d, 1H), 9.26(s, 1H)

Embodiment 2

[0052] [Example 2] Preparation of tert-butylcarbonyloxymethyl-(Z)-3[4-(1H-imidazolyl-1-methyl)phenyl]-2-acrylate.

[0053] Put 22.8g of ozagrel into 120ml of DMA, add 5.5g of sodium isooctanoate and 10ml of water under stirring, stir at 10-15°C for 30 minutes, cool to 0-5°C, add 15.8g of tert-butylcarbonyloxymethane, React at 10-15°C for 2 hours, pour into 200ml of ethyl acetate, then add 100ml of 5% sodium bicarbonate solution, stir, separate the organic phase, extract the aqueous phase with 20ml of ethyl acetate, combine ethyl acetate, anhydrous Dry over magnesium sulfate, filter, and evaporate the solvent under reduced pressure to obtain 27.4 g of white to off-white powder (yield 80%).

[0054] 1 H-NMR (CD 3 Cl, δ) 1.31(s, 9H), 4.96(s, 2H), 6.42(d, 1H), 6.94(s, 2H), 7.15-7.26(m, 6H), 7.68(d, 1H), 9.30(s , 1H)

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Abstract

The invention discloses an ozagrel ester with the compounds of the ozagrel ester. The ozagrel ester is provided with a chemical structural formula as listed on the right. The compounds of the ozagrel ester comprise an ozagrel ester with the amount of effective treatment and a carrier accepted in medicine. The invention also discloses the preparation methods for the ozagrel ester and the compounds of the ozagrel ester. The ozagrel ester of the invention has good solubility and stability; besides, the compounds of ozagrel ester can be conveniently made into a plurality of liquid, solid, freeze-drying and mucosa or the skin medication agents.

Description

technical field [0001] The invention relates to an ozagrel ester and a preparation thereof, in particular to an ozagrel ester, a composition and a preparation method thereof. Background technique [0002] Ozagrel, namely trans 3-[4-(1H-imidazole-1-methyl)phenyl]-2-acrylic acid, is a highly effective and powerful inhibitor of thromboxane (TXA2) synthetase, which can specifically inhibit Thromboxane synthase, which reduces the production of thromboxane synthase, has the effect of anti-platelet aggregation and relieving vasospasm, can inhibit cerebral thrombosis and cerebral vasospasm, and can be used for the improvement of cerebral ischemic symptoms after subarachnoid hemorrhage surgery. [0003] At present, ozagrel sodium injection formulations are often used clinically, but according to literature reports, ozagrel is unstable in aqueous solution and can be partially isomerized and converted into cis-imidazole methyl cinnamic acid, which reduces its curative effect. [0004]...

Claims

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Application Information

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IPC IPC(8): C07D233/60A61K31/4174A61K9/00A61P7/02A61P9/10
Inventor 王立峰
Owner 王立峰
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