Ornithine and aspartate compound and novel method thereof

A technology of ornithine aspartate and aspartic acid, applied in the field of medicine, can solve the problems of high cost, inconvenient synthesis and the like

Inactive Publication Date: 2010-11-10
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This patent mainly uses D403 chelating resin to remove barium ions, which is cos

Method used

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  • Ornithine and aspartate compound and novel method thereof
  • Ornithine and aspartate compound and novel method thereof
  • Ornithine and aspartate compound and novel method thereof

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Experimental program
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Effect test

Embodiment 1

[0018] The preparation of embodiment 1 aspartic acid ornithine

[0019] Dissolve 384g of L-ornithine acetate in 500ml of water, then adjust the pH of the system to 7.5 with ammonia water, add 3L of acetone, stir at room temperature for 2 hours to completely precipitate ammonium acetate, filter, and concentrate the filtrate under reduced pressure to 400ml, then add 266g of L-aspartic acid, stir and heat up to 60°C, slowly add 800ml of methanol, the solution starts to become cloudy, then heat and reflux the solution for 40 minutes, then cool to room temperature, filter to obtain a white solid, and then The white solid was added to 900ml of methanol, heated to reflux for beating, cooled to room temperature, filtered, and vacuum-dried at 50°C to obtain 453g of ornithine aspartate with a yield of 85.4%, a purity of 99.5%, and a specific rotation [α] D 20 ° = 26.7°.

Embodiment 2

[0020] The preparation of embodiment 2 aspartic acid ornithine

[0021] Dissolve 384g of L-ornithine acetate in 500ml of water, then adjust the pH of the system to 7.0 with ammonia water, add 3L of acetone, and stir at room temperature for 4 hours to completely precipitate ammonium acetate, filter, and concentrate the filtrate under reduced pressure to 400ml, then add 266g of L-aspartic acid, stir and heat up to 50°C, slowly add 700ml of methanol, the solution starts to become cloudy, then heat the solution to reflux for 20 minutes, then cool to room temperature, filter to obtain a white solid, and then The white solid was added to 800ml of methanol, heated to reflux for beating, cooled to room temperature, filtered, and vacuum-dried at 60°C to obtain 448g of ornithine aspartate with a yield of 84.4%, a purity of 99.6%, and a specific rotation [α] D 20 ° = 26.6°.

Embodiment 3

[0022] The preparation of embodiment 3 aspartic acid ornithine

[0023] Dissolve 384g of L-ornithine acetate in 500ml of water, then adjust the pH of the system to 8.0 with ammonia water, add 3L of acetone, and stir at room temperature for 3 hours to completely precipitate the ammonium acetate, filter, and concentrate the filtrate under reduced pressure to 400ml, then add 266g of L-aspartic acid, stir and heat up to 55°C, slowly add 700ml of methanol, the solution starts to become cloudy, then heat the solution to reflux for 30 minutes, then cool to room temperature, filter to obtain a white solid, and then The white solid was added to 800ml of methanol, heated to reflux for beating, cooled to room temperature, filtered, and vacuum-dried at 55°C to obtain 465g of ornithine aspartate with a yield of 87.6%, a purity of 99.5%, and a specific rotation [α] D 20 ° = 26.7°.

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Abstract

The invention relates to an ornithine aspartate compound and a novel method thereof. L-aspartic acid and L-ornithine acetate are used as starting materials. The method comprises the following steps of: removing ammonium acetate serving as an intermediate product through solubility differences of ornithine and the ammonium acetate in acetone to obtain free alkali of the ornithine; and reacting thefree alkali with the L-aspartic acid to generate the ornithine and aspartate compound. The synthetic method of the ornithine and aspartate compound has the advantages of low cost, simple process, high purity of the obtained product and easy industrial production.

Description

technical field [0001] The invention relates to an aspartic acid ornithine compound and a new method thereof, belonging to the technical field of medicine. Background technique [0002] Ornithine Aspartate, the chemical name is (S)-2,5-diaminovaleric acid-(S)-2-aminosuccinate, and the molecular formula is C 9 h 19 N 3 o 6 , the molecular weight is 265.27, and the structural formula is: [0003] [0004] Ornithine aspartate is an essential substance that provides urea and glutamine synthesis. Glutamine is the detoxification product of ammonia, and it is also the storage and transportation form of ammonia; under physiological and pathological conditions, the synthesis of urea and the synthesis of glutamine will be affected by ornithine, aspartic acid and other dicarboxylic compounds. influences. Ornithine is almost involved in the activation of urea cycle and the whole process of ammonia detoxification. In the process, arginine is formed, which in turn splits off ure...

Claims

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Application Information

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IPC IPC(8): C07C229/26C07C227/18
Inventor 王明
Owner HAINAN LINGKANG PHARMA CO LTD
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