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Polyunsaturated fatty acyl phosphatide derivative and preparation method and application thereof

A technology of fatty acyl phospholipids and derivatives, which is applied in the field of series derivatives of compounds, can solve the problems such as great difference in drug efficacy, and achieve the effect of novel structure, convenient operation and prevention of fat accumulation

Inactive Publication Date: 2015-09-16
THIRD INST OF OCEANOGRAPHY STATE OCEANIC ADMINISTATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although phospholipids and existing polyunsaturated fatty acylphospholipids have certain blood lipid-lowering activities, their efficacy is far from that of existing blood lipid-lowering drugs, so they have not been developed into pharmaceutical preparations

Method used

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  • Polyunsaturated fatty acyl phosphatide derivative and preparation method and application thereof
  • Polyunsaturated fatty acyl phosphatide derivative and preparation method and application thereof
  • Polyunsaturated fatty acyl phosphatide derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: prepare DHA-PC (2) compound (2a), the structural formula of compound (2a) is:

[0042]

[0043] Mix 12mmol polyunsaturated fatty acid and 10mmol phosphorylated ethanolamine evenly, and slowly drop into the ester condensing agent, which includes 1.4mL DMF, 3.6mL Et 3 N and 1.2 mL (COCl) 2 30mL dichloromethane mixed solution, stirred at 0°C for 2h. After the reaction finished, the reaction solution was added with saturated sodium carbonate solution (100mL), extracted twice with dichloromethane (50mL), dried over anhydrous magnesium sulfate, concentrated under reduced pressure after filtration, and the thick product was subjected to quick silica gel column chromatography (V 乙酸乙酯 :V 石油醚 =1:2), and purified to obtain a yellow viscous product. Agilent XDB-C18ZORBAX HPLC for further purification, room temperature, mobile phase (V 甲醇 :V 水 =95:5), flow rate 20ml / min, collection retention time t 1 / 2 = the component of 6.1min, promptly obtains light yellow vis...

Embodiment 2

[0046] Embodiment 2: prepare DHA-PC (3) compound (2b), the structural formula of compound (2b) is:

[0047]

[0048] Mix 12mmol polyunsaturated fatty acid and 10mmol phosphorylated propanolamine evenly, and slowly drop into the ester condensing agent, which includes 1.2mL DMF, 3.0mL Et 3 N and 1.0 mL (COCl) 2 30mL dichloromethane mixed solution, stirred at 0°C for 2h. After the reaction finished, the reaction solution was added with saturated sodium carbonate solution (100mL), extracted twice with dichloromethane (50mL), dried over anhydrous magnesium sulfate, concentrated under reduced pressure after filtration, and the thick product was subjected to quick silica gel column chromatography (V 乙酸乙酯 :V 石油醚 =1:2), and purified to obtain a yellow viscous product. Agilent XDB-C18ZORBAX HPLC for further purification, room temperature, mobile phase (V 甲醇 :V 水 =95:5), flow rate 20ml / min, collection retention time t 1 / 2 = 5.9min component, that is, a light yellow viscous produ...

Embodiment 3

[0051] Embodiment 3: prepare DHA-PC (4) compound (2c), the structural formula of compound (2c) is:

[0052]

[0053] Mix 12mmol polyunsaturated fatty acid and 10mmol phosphorylated butanolamine evenly, and slowly drop into the ester condensing agent, which includes 1.6mL DMF, 4.2mL Et 3 N and 1.4 mL (COCl) 2 30mL dichloromethane mixed solution, stirred at 0°C for 2h. After the reaction finished, the reaction solution was added with saturated sodium carbonate solution (100mL), extracted twice with dichloromethane (50mL), dried over anhydrous magnesium sulfate, concentrated under reduced pressure after filtration, and the thick product was subjected to quick silica gel column chromatography (V 乙酸乙酯 :V 石油醚 =1:2), and purified to obtain a yellow viscous product. Agilent XDB-C18ZORBAX HPLC for further purification, room temperature, mobile phase (V 甲醇 :V 水 =95:5), flow rate 20ml / min, collection retention time t 1 / 2 = 6.6min component, that is, a light yellow viscous produc...

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Abstract

The invention discloses a polyunsaturated fatty acyl phosphatide derivative and a preparation method and application thereof, the structural formula of the derivative is shown in the specification, wherein m = 5 or 6; n = 2, 3 or 5; k = 2, 3, 4, 5 or 6; and the polyunsaturated fatty acyl phosphatide derivative is prepared by evenly mixing polyunsaturated fatty acid and phosphoryl alcohol amine under the action of an ester condensation agent. The polyunsaturated fatty acyl phosphatide derivative not only can inhibit fat absorption, promotes the function of fat hydrolysis, but also can promote the fat hydrolysis and prevent fat accumulation, meanwhile does not affect the patient's appetite, and can be developed into drugs for reducing blood fat, regulating eating disorders, treating nutritional diseases such as being overweight or obese and the like.

Description

technical field [0001] The present invention relates to a series of derivatives of compounds, in particular to a polyunsaturated fatty acyl phospholipid derivative and its preparation method and application, and the series of polyunsaturated fatty acyl phospholipid derivatives are used in the preparation of drugs for regulating blood lipids, Applications in health care products or food. Background technique [0002] The improvement of material living conditions and the change of lifestyle have led to an increase in the incidence of hyperlipidemia year by year, and nutritional and metabolic diseases caused by hyperlipidemia, such as dyslipidemia and atherosclerosis, have become serious threats to human health. A class of diseases. According to a survey report on obesity in various countries released by the World Health Organization, the report shows that at least 1.6 billion people in the world are overweight or obese. [0003] Phospholipids (PC) are a class of phospholipid...

Claims

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Application Information

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IPC IPC(8): C07F9/24A61K31/664A61P3/06A61P3/04A23L1/30
Inventor 方华黄晓燕陈伟珠谢全灵张怡评洪专
Owner THIRD INST OF OCEANOGRAPHY STATE OCEANIC ADMINISTATION
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