A kind of preparation method of synthetic phospholipid DPPC

A technology for synthesizing phospholipids and palmitoyl phosphatidyl choline, which is applied in the field of medicine and chemical industry, can solve the problems of cumbersome post-processing process, high toxicity of reaction solvent, serious environmental pollution, etc., and achieves the advantages of cheap raw materials, easy industrial production and high economic benefits. Effect

Active Publication Date: 2018-01-12
苏州东南药业股份有限公司
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Problems solved by technology

[0006] The technical problem to be solved by the present invention is in order to overcome the severe reaction conditions of the preparation method of existing dipalmitoylphosphatidylcholine, the toxicity of the reaction solvent is large, the post-treatment process is loaded down with trivial details, the environmental pollution is serious, the reaction conversion rate is low, and the yield is low. Low, high production cost, unsuitable for defects such as industrialized production, but a kind of preparation method and application of dipalmitoylphosphatidylcholine are provided. , the reaction to obtain dipalmitoylphosphatidylcholine, the raw material is cheap, the reaction conditions are mild, the operation is safe, the post-treatment operation is simple, the yield is high, and it is suitable for large-scale production

Method used

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  • A kind of preparation method of synthetic phospholipid DPPC
  • A kind of preparation method of synthetic phospholipid DPPC
  • A kind of preparation method of synthetic phospholipid DPPC

Examples

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Embodiment 1

[0029] Add 50g glycerylphosphonocholine, 200g palmitic acid, 95g DMAP, and 1000mL chloroform to a clean and dry 2000mL three-necked flask. Stir evenly with magnetic force, and protect with argon replacement. Dissolve 165 g of DCC with 1000 mL of chloroform, and quickly drop the DCC chloroform solution into the reaction system. Avoid light and react at 20°C for 5h. During the reaction process, a large amount of white insoluble solids appeared, and the reaction was stopped if no further progress was detected by TLC. The reaction solution was filtered to remove the white insoluble solid DCU to obtain a bright yellow transparent liquid, which was evaporated to dryness to obtain a yellow viscous liquid, which was beaten with 3000 mL of acetone for 10 h, and a large amount of white solids were precipitated in the system. The catalyst 4-dimethylaminopyridine (DMAP) in the system was removed by filtration. Repeat once, filter off-white solid, and dry to obtain crude product 130g. ...

Embodiment 2

[0033] Add 5g glycerylphosphonocholine, 20g palmitic acid, 9.5g TEA, and 50mL chloroform into a clean and dry 200mL three-necked flask. Stir evenly with magnetic force, and protect with argon replacement. 16.5 g of DCC was dissolved in 200 mL of chloroform, and the DCC chloroform solution was quickly dropped into the reaction system. Protect from light and react below 20°C for 1d. During the reaction process, a large amount of white insoluble solids appeared, and the reaction was stopped if no further progress was detected by TLC. The reaction solution was filtered to remove the white insoluble solid DCU to obtain a bright yellow transparent liquid, which was evaporated to dryness to obtain a yellow viscous liquid, which was beaten with 300 mL of acetone for 10 hours, and a large amount of white solid was precipitated in the system, filtered to obtain an off-white solid, and dried to obtain Crude product 13g. Heat the crude product with 200mL of dichloromethane at 50°C with...

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Abstract

The invention provides a method for artificially synthesizing phospholipid DPPC (dipalmitoyl phosphatidylcholine).The target product, DPPC, is synthesized from glyceryl phosphoryl choline and palmitic acid through condensation reaction.The method is simple in step, mild in reaction and suitable for industrial production.The prepared DPPC can be used for various medicines such as injection, tablets and capsules as a pharmaceutical adjuvant.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a process preparation method and application of synthesizing phospholipid dipalmitoylphosphatidylcholine. Background technique [0002] Phospholipids are an important part of biological membranes. The polar ends containing phosphate groups are hydrophilic, and the nonpolar ends of the two longer hydrocarbon chains are lipophilic. This unique physical and chemical property enables them to spontaneously dissolve in water. A closed bilayer is formed in the medium, which becomes the skeleton of the biomembrane, and phospholipids play a vital role in liposome technology. Liposomes were first discovered by the British scholar Bangham when phospholipids were dispersed in water and observed under an electron microscope. In 1971, British Lyman et al. used liposomes as drug carriers. However, as liposome materials, natural phospholipids have disadvantages such as ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/10
CPCC07F9/10
Inventor 宗玺吉民李锐顾惠龙刘海东曹萌
Owner 苏州东南药业股份有限公司
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