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Novel method for synthesizing bi-axungia acyl-phosphatidylethanolamine

A technology of stearoyl phosphatidylethanolamine and palmitoyl phosphatidylethanolamine, which is applied in the direction of phosphorus organic compounds, etc., to achieve the effects of simplifying the process, reducing production costs, and simple synthesis methods

Active Publication Date: 2012-01-04
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to overcome the deficiencies such as complex reaction conditions, cumbersome operation and low yield in the prior art, and provide a compound di-fatty acylphosphatidylethanolamine (I) new preparation method

Method used

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  • Novel method for synthesizing bi-axungia acyl-phosphatidylethanolamine
  • Novel method for synthesizing bi-axungia acyl-phosphatidylethanolamine
  • Novel method for synthesizing bi-axungia acyl-phosphatidylethanolamine

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 2: Preparation of dipalmitoylphosphatidylethanolamine

[0020] Dissolve 2g (0.0035mol) dipalmitoylglyceride, 1.34g (0.0087mol) phosphorus oxychloride, 1.21g (0.012mol) triethylamine in 24 chloroform solution, control the temperature at 35 degrees, then react for 2h, react After stopping, filter and concentrate the filtrate to obtain a concentrated solution, then react with 0.55g (0.009mol) ethanolamine and 2.42g (0.024mol) triethylamine in 20ml tetrahydrofuran solution at a temperature of 20 degrees, react for 15min, filter, and concentrate the filtrate. get crude. The crude product was purified with cyclohexane to obtain 2.1 g of dipalmitoylphosphatidylethanolamine. 1 H-NMR (CDCl 3 , δppm): 0.88 (6H, t), 1.23-1.27 (48H, m), 1.64 (4H, d), 2.27-2.32 (4H, m), 3.22-3.26 (2H, m), 4.1 (2H, d ), 4.12-4.19 (3H, m), 4.36-4.38 (1H, m), 5.23 (1H, s), 8.33 (3H, s).

Embodiment 2

[0021] Embodiment 3: Preparation of Dimyrisyl Phosphatidylethanolamine

[0022] Dissolve 2g (0.004mol) of digicolithylglyceride, 1.23g (0.008mol) of phosphorus oxychloride, and 1.01g (0.01mol) of triethylamine in 14ml of trichloroethylene solution at a temperature of 20 degrees, then react for 4 hours, and react After stopping, filter and concentrate the filtrate to obtain a concentrate, then react with 0.49g (0.008mol) ethanolamine and 2.02g (0.02mol) triethylamine in 12ml of chloroform solution at a temperature of 15°C for 30min, filter and concentrate the filtrate. get crude. The crude product was refined with petroleum ether to obtain 1.96 g of dimyrisylphosphatidylethanolamine. 1 H-NMR (CDCl 3 , δppm): 0.89 (6H, t), 1.24-1.27 (40H, m), 1.60 (4H, d), 2.20-2.32 (4H, m), 3.21-3.23 (2H, m), 4.0 (2H, d ), 4.10-4.16 (3H, m), 4.36-4.38 (1H, m), 5.23 (1H, s), 8.33 (3H, s).

Embodiment 3

[0023] Embodiment 4: Preparation of dipalmitoylphosphatidylethanolamine

[0024] Dissolve 2g (0.0035mol) of dipalmitoylglyceride, 0.97g (0.0063mol) of phosphorus oxychloride, and 0.71g (0.007mol) of triethylamine in 10ml of trichloroethylene solution and 4ml of dichloromethane, and control the temperature at 0 degree, then reacted for 5.5h, after the reaction stopped, filtered, and the filtrate was concentrated to obtain a concentrated solution, which was then reacted with 0.43g (0.007mol) ethanolamine and 1.01g (0.01mol) triethylamine in 14ml dichloromethane solution, and the temperature was 5 degree, reacted for 35min, filtered, and the filtrate was concentrated to obtain a crude product. The crude product was refined with n-hexane to obtain 2.08 g of dipalmitoylphosphatidylethanolamine. HPLC: 98.1%.

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Abstract

The present invention relates to a method for preparing di-fatty acyl phosphatidylethanolamine as an accessory used in the technology of lipidosomes. In the preparation method, di-fatty acyl glyceride is used as starting material, which is finally reacted with phosphorus oxychloride and neovaricaine to produce the compound, di-fatty acyl phosphatidylethanolamine.

Description

technical field [0001] The invention relates to a new synthesis method of difatty acylphosphatidylethanolamine as an auxiliary material used in liposome technology. Background technique [0002] Liposomes were first discovered by British scholar Bangham when he dispersed phospholipids in water for electron microscope observation. Phospholipids are dispersed in water to form multilayered vesicles, and each layer is a lipid bilayer. Later, this bimolecular vesicle with a structure similar to a biological membrane is called a liposome. In 1971, British Liman and others began to use liposomes as drug carriers. Since then, liposome, as a new dosage form of targeted drug delivery system, has attracted worldwide attention. [0003] Phospholipids play an important role in liposome technology, and phospholipids include natural phospholipids and synthetic phospholipids. Difatty acylphosphatidylethanolamine (I) belongs to a kind of in synthetic phospholipid, wherein RCOO in the com...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/09
Inventor 王金戌吴立红孟程军郑利刚陈玉洁刘亚英
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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