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Method for preparing citicoline sodium

A kind of technology of citicoline sodium and phosphorylcholine chloride

Active Publication Date: 2014-09-10
安庆回音必制药股份有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] ① Chemical synthesis, using CMP (5'-cytidylic acid) and phosphorylcholine as reactants, p-toluenesulfonyl chloride as condensation agent, condensation preparation in the presence of N-dimethylformamide, using 717 (Cl- ) type anion exchange column and 711 (Cl-) type concentrated column separation liquid alcohol precipitation to prepare citicoline sodium, its shortcoming is that it is difficult to separate from the condensing agent, and the product is not suitable for medicinal use;
[0013] ②Enzymatic synthesis, extracting cell fluid to biosynthesize citicoline sodium with cytidine triphosphate (CTP) and phosphorylcholine, the synthesis of enzyme and cell extract requires substrate CTP, and the synthesis price is high;
[0014] ③Citicoline sodium is synthesized by free cells and yeast cell-free extracts. The synthesis of free yeast requires a large amount of yeast and can only be used once, which has many disadvantages

Method used

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  • Method for preparing citicoline sodium
  • Method for preparing citicoline sodium

Examples

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Embodiment 1

[0040] Put 2.58kg of phosphoric acid choline calcium salt into a 50L neutralization reaction pot, add 10L of water, heat up to 50°C, stir and dissolve, add 1kg of oxalic acid (calculated as anhydrous matter), and precipitate a white precipitate, keep stirring for 0.5 hours, Cool to 0-10°C, centrifuge to remove the precipitate, pump the filtrate into a 100L still, add 1L of benzene, distill under reduced pressure to remove water and benzene, add 8L of tetrahydrofuran to the remaining viscous material to dissolve, and obtain intermediate liquid 1.

[0041] Add 0.8 kg of solid phosgene dissolved in 10 L of tetrahydrofuran and 50 ml of DMF into a dry reaction kettle, stir at room temperature, drop in intermediate material liquid 1, and react for 0.5 hours, then add 2.5 kg of cytidylic acid, stir and react at room temperature for 5 hours, reduce Recover the solvent by pressure.

[0042] Add 5L of sodium hydroxide 20% aqueous solution to the residue and heat up to 80°C to dissolve, ...

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Abstract

The invention discloses a method for preparing citicoline sodium. The method comprises the following steps: adding oxalic acid into a chlorination calcium water solution, removing the precipitate and water, reacting with cytidine monophosphate under the action of triphosgene, and subsequently purifying the citicoline sodium by using a recrystallization method.

Description

technical field [0001] The invention relates to a method for preparing the compound citicoline sodium, which belongs to the technical field of biopharmaceuticals. Background technique [0002] Citicoline sodium, also known as citicoline sodium, is an activator of brain metabolism. As an intermediate in the endogenous synthesis of phosphatidylcholine, it can promote the synthesis of phospholipids in nerve cell membranes. Phospholipids are also important components for building biological membranes. . [0003] After the central nervous system is injured, citicoline sodium participates in the repair and regeneration and plays a neuroprotective role; it also plays an important role in the transfer of nerve media and the conduction of bioelectricity. Citicoline sodium is mainly used clinically for head trauma and brain surgery accompanied by disturbance of consciousness, acute disturbance of consciousness in cerebral infarction, promoting the recovery of upper limb function in p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/02
Inventor 王大冲王建蒋叔霏
Owner 安庆回音必制药股份有限公司
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