Method for synthesizing phosphatidylcholine by using solid-phase carrier

A technology for synthesizing phosphatidylcholine and phosphatidylcholine, which is applied in the field of medicine and chemical industry, can solve the problems of unsuitability for industrial production, harsh preparation method conditions, cumbersome post-processing procedures, etc., and achieve easy large-scale industrial production and increase molecular collisions chance, the effect of increasing the reaction surface area

Pending Publication Date: 2022-02-08
江苏东南纳米材料有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention overcomes the defects of the existing phosphatidylcholine preparation method, such as harsh conditions, cumbersome post-treatment procedures, serious environmental pollution, low reaction conversion rate, low yield, high production cost and unsuitability for industrialized production, and provides A method for solid-phase synthesis of phosphatidylcholine, using activated carbon as a solid-phase adsorption material, evenly adsorbing glycine phosphatidylcholine, and then acylation reaction with fatty acid chloride to obtain phosphatidylcholine

Method used

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  • Method for synthesizing phosphatidylcholine by using solid-phase carrier
  • Method for synthesizing phosphatidylcholine by using solid-phase carrier
  • Method for synthesizing phosphatidylcholine by using solid-phase carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0039] (1) Add 51.4g glycerol phosphorylcholine into a clean and dry 3000ml three-necked bottle with mechanical stirring, replace nitrogen, start stirring, heat until glycerol phosphorylcholine melts, and add different adsorbents (adsorbent selection From activated carbon, aluminum oxide, silica gel, diatomaceous earth) 154.2g, continue to stir for 1 hour, make glycerol phosphorylcholine fully and evenly adsorbed by the adsorbent.

[0040] (2) Cool down to room temperature, add 1500 mL of chloroform and 60.7 g of triethylamine, add 181.75 g of stearyl chloride dropwise at a temperature of 20°C, after the addition is complete, keep stirring for 1 hour, heat up to 30-35°C, filter, Transfer the filtrate to a clean and dry 3000ml three-neck flask with mechanical stirring, start the stirring, cool down to -5~5°C for crystallization for 3~4 hours, filter, rinse the filter cake with a small amount of ice chloroform, drain it, and dry it in vacuum for 24 hours. Hours, DSPC137.5g was o...

Embodiment 2

[0049] (1) Add 51.4g of glycerol phosphorylcholine into a clean and dry 3000ml three-necked bottle with mechanical stirring, replace the nitrogen, start stirring, heat until the glycerol phosphorylcholine melts, add 154.2g of activated carbon under stirring, and continue stirring for 1 hour , so that glycerol phosphorylcholine is fully and evenly adsorbed by activated carbon.

[0050](2) Cool down to room temperature, add 1500 mL of chloroform and 60.7 g of triethylamine, add 164.92 g of palmitoyl chloride dropwise under temperature control at 20°C, after the addition is complete, keep stirring for 1 hour, heat up to 30-35°C, filter, and the filtrate Transfer to a clean and dry 3000ml three-neck flask with mechanical stirring, turn on the stirring, cool down to -5~5°C to crystallize for 3~4 hours, filter, rinse the filter cake with a small amount of ice chloroform, drain, and vacuum dry for 24 hours , to obtain DPPC 130.1g, yield 88.6%.

[0051] the resulting product, 1 H-NM...

Embodiment 3

[0053] (1) Add 51.4g of glycerol phosphorylcholine into a clean and dry 3000ml three-necked bottle with mechanical stirring, replace the nitrogen, start stirring, heat until the glycerol phosphorylcholine melts, add 154.2g of activated carbon under stirring, and continue stirring for 1 hour , so that glycerol phosphorylcholine is fully and evenly adsorbed by activated carbon.

[0054] (2) Cool down to room temperature, add 1500 mL of chloroform and 60.7 g of triethylamine, add 214.21 g of erucic acid chloride dropwise at a temperature of 20°C, after the addition is complete, keep stirring for 1 hour, heat up to 30-35°C, and filter. Transfer the filtrate to a clean and dry 3000ml three-neck flask with mechanical stirring, start the stirring, cool down to -10-0°C to crystallize for 3-4 hours, filter, rinse the filter cake with a small amount of ice chloroform, drain it, and dry it in vacuum for 24 hours. Hours, DEPC 154.7g was obtained with a yield of 86.1%.

[0055] the result...

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Abstract

The invention provides a method for artificially synthesizing phosphatidylcholine by using a solid-phase carrier, which comprises the following steps of: melting choline glycerophosphate, uniformly adsorbing the melted choline glycerophosphate with activated carbon, carrying out acylation reaction with fatty acid acyl chloride, and filtering and recrystallizing the obtained product to obtain high-purity phosphatidylcholine. The phosphatidylcholine prepared by the method disclosed by the invention can be used as a pharmaceutical adjuvant for various medicines such as injections, tablets and capsules.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a method and application for synthesizing phosphatidylcholine by using a solid phase carrier. Background technique [0002] Phospholipids are an important part of biological membranes. The polar end containing phosphate is hydrophilic, and the non-polar ends of the two longer hydrocarbon chains are lipophilic. This unique physical and chemical property enables it to rehydrate spontaneously. A closed bilayer is formed in the medium and becomes a biomembrane skeleton, and phospholipids play a vital role in liposome technology. However, as liposome materials, natural phospholipids have disadvantages such as short lifespan, easy oxidation, and poor stability, which limit their application. [0003] Phosphatidylcholine is an important synthetic phospholipid, which is mainly used in the preparation of liposomes and is an indispensable additive excipient in lip...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/10
CPCC07F9/10
Inventor 于文渊吉民王冬冬刘来富胡海燕
Owner 江苏东南纳米材料有限公司
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