Preparation method of dioleoyl phosphatidylcholine
A technique for dioleoylphosphatidylcholine and a purification method, which is applied in the field of preparation of phospholipid dioleoylphosphatidylcholine, can solve the problems of harsh preparation conditions, cumbersome post-treatment procedures, and low reaction conversion rate, and achieve Ease of large-scale industrial production, cheap raw materials, and high purification efficiency
Pending Publication Date: 2020-07-28
苏州东南药业股份有限公司 +1
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Problems solved by technology
[0005] The technical problem to be solved by the present invention is to overcome the harsh conditions of the existing dioleoylphosphatidylcholine preparation method, cumbersome post-treatment procedures, serious environmental pollution, low reaction conversion rate, low yield, and high production cost , is not suitable for the defect of industrialized production, a kind of preparation method of dioleoylphosphatidylcholine is provided, the present invention directly reacts glycerol phosphorylcholine and oleic acid under the action of alkali and condensing agent to obtain dioleoylphosphatidylcholine Acylcholine, cheap raw materials, mild reaction conditions, safe operation, simple post-treatment, high yield, suitable for industrial production
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Embodiment 1
[0031] (1) Add 50g glycerophosphorylcholine, 220g oleic acid, 95g DMAP, and 1000mL chloroform into a clean and dry 3000ml three-necked flask. Magnetically stir evenly. Dissolve 165 g of DCC in 1000 mL of chloroform, and quickly drop the DCC chloroform solution into the reaction system. Protected from light and reacted at 20°C for 12h. A large amount of white solid was produced, and the TLC detection reaction showed no further progress, so the reaction was stopped. Concentrate to dryness to obtain a yellow viscous liquid.
[0032] (2) Add solvent 1 acetone, beating and stirring for 3 hours, a large amount of solids are precipitated, and the crude product is obtained by drying. Heat the crude product with 1000ml of solvent 2 dichloromethane to 40°C and stir to dissolve, filter while hot to remove insoluble matter, cool the filtrate to 0°C, slowly add 1800mL of solvent 3 methyl tert-butyl ether dropwise, the system gradually becomes cloudy, slowly stirring has A large number ...
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The invention provides a method for artificially synthesizing dioleoyl phosphatidylcholine (DOPC), which comprises the following steps of: using glycerol phosphatidylcholine and oleic acid as raw materials to carry out a condensation reaction, pulping the obtained product, filtering, and recrystallizing to obtain high-purity dioleoyl phosphatidylcholine. The dioleoyl phosphatidylcholine (DOPC) prepared by the method disclosed by the invention can be used as a pharmaceutic adjuvant for various types of medicines such as injections, tablets, capsules and the like.
Description
technical field [0001] The invention belongs to the field of medicine and chemical industry, in particular to a preparation method and application of synthesizing phospholipid dioleoylphosphatidylcholine. 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. Liposomes were first discovered by British scholar Bangham when phospholipids were dispersed in water and observed under an electron microscope. In 1971, British Liman et al. used liposomes as drug carriers. However, as liposome materials, natural phospholipids have disadvantages such as short lifespan, easy oxidation, and poor stability, which...
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Login to View More IPC IPC(8): C07F9/10
CPCC07F9/10
Inventor 于文渊吉民宗玺胡海燕齐伟张影
Owner 苏州东南药业股份有限公司