Method for preparing citicoline sodium by utilizing oxalyl chloride

A technology of citicoline sodium and oxalyl chloride, applied in the field of biopharmaceuticals, can solve the problems of high synthesis price, only one-time use, a large amount of yeast, etc., and achieves a good atomic economy, simple operation process, and improved yield. Effect

Active Publication Date: 2014-08-27
回音必集团抚州制药有限公司
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AI Technical Summary

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 by utilizing oxalyl chloride

Examples

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Comparison scheme
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Embodiment 1

[0031] Put 2.58 kg of calcium phosphoric acid choline chloride into a 50L neutralization reaction pot, add 10L of pyridine and 0.5L of benzene, heat to reflux, and separate the water with a water separator. Cool to room temperature.

[0032] Add 0.8 kg of oxalyl chloride to the reaction pot, react for 1 hour, add 10 L of THF solution containing 2.5 kg of cytidylic acid, and stir and react at room temperature for 5 hours. The solvent was recovered under reduced pressure.

[0033] The remaining viscous material was added to 5L of a mixed solution containing 10% sodium hydroxide and 10% sodium carbonate, heated and stirred, and the insoluble matter was filtered off. After adding 60 g of activated carbon to the solution and stirring for 30 min to decolorize, filter. Add 20L of absolute ethanol to the filtrate while stirring and cooling to 0°C, let it stand for 12 hours to precipitate all the solids, and centrifuge to obtain the product. After drying at 100°C, 4.3Kg of solid was...

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Abstract

The invention discloses a method for preparing citicoline sodium by utilizing oxalyl chloride. The method is characterized by comprising the following steps of: by taking choline chloride calcium phosphate (P-choline) as a raw material, dissolving in organic amine not containing reactive hydrogen, adding oxalyl chloride for reacting for 0.5-2 hours after adding benzene for removing water in an azeotropic manner, and then, adding cytidylic acid (5'-CMP) for reacting.

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): C07H19/10C07H1/00
Inventor 余中华
Owner 回音必集团抚州制药有限公司
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