Method for preparing 5'-cytidylic acid from composite solvent and bind acid agent

A composite solvent and acid-binding agent technology, applied in chemical instruments and methods, preparation of sugar derivatives, sugar derivatives, etc., can solve problems such as unstable product quality, achieve high selectivity and speed up the effect

Inactive Publication Date: 2011-10-12
NANTONG SANE BIOLOGICAL
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  • Abstract
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Problems solved by technology

The current method for making 5'-cytidylic acid usually adopts the method of microbial synthesis. Although it has a certain scale, the yield is only about 85%, and the quality of the product is not stable. The ultraviolet content is about 97%, and the HPLC content is about About 97.5%

Method used

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Embodiment 1

[0013] Embodiment 1: A method for making 5'-cytidylic acid using a composite solvent and an acid-binding agent, has the following steps:

[0014] (1) Prepare composite solvent: the composite solvent contains sulfoxide solvent and tri-lower alkyl phosphate, and the ratio of sulfoxide solvent to tri-lower alkyl phosphate is 50g:500g. During the reaction, a sulfoxide solvent and a tri-lower alkyl phosphate are used as a composite solvent, which utilizes the property that the composite solvent can increase the solubility or dissolution rate of the solute to ensure that there is no interference in the next reaction, that is, the reaction has a directional property, specifying the introduction of a phosphate group at the 5'-position of cytidine upon phosphorylation of cytidine.

[0015] (2) Adding phosphorylating agent: the phosphorylating agent is phosphorus oxyhalide, and phosphorus oxyhalide is phosphorus oxychloride or phosphorus oxybromide. The non-interfering reaction is carr...

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PUM

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Abstract

The invention relates to a method for preparing 5'-cytidylic acid from a composite solvent and a bind acid agent. The method comprises the following detailed steps of: (1) preparing the composite solvent which contains a sulfoxide solvent and alkyl three-low level phosphate; (2) adding a phosphorylation agent, namely at the temperature of -2 to 2 DEG C, dropwise adding the phosphorylation agent into the composite solvent to perform an intervention reaction, wherein the phosphorylation agent and a certain amount of water in the composite solvent react to generate a part of hydrate; (3) adding cytidine, namely gradually adding the cytidine at the temperature of 0 to 5 DEG C to perform reaction for 3 to 5 hours; and (4) adding the bind acid agent, namely adding the phosphorylation agent and the bind acid agent in a proportion of 100:0.8-100:0.6. The yield of the product obtained by the method is over 90 percent; the ultraviolet content of the generated 5'-cytidylic acid is over 98 percent; and the high-performance liquid chromatography (HPLC) content of the generated 5'-cytidylic acid is over 98 percent.

Description

technical field [0001] The invention relates to a method for producing 5'-cytidylic acid, in particular to a method for producing 5'-cytidylic acid by using a composite solvent and an acid-binding agent. Background technique [0002] Cytidylic acid, English name: cytidylic acid, is the phosphate ester of cytidine. Depending on the phosphoric acid linking site, there are cytidine 2'-phosphate (2'-cytidylic acid), cytidine 3'-phosphate (3'-cytidylic acid) and cytidine 5'-phosphate (5'-cytidylic acid ) three kinds. Cytidylic acid in the body is usually 5'-cytidylic acid. The current method for making 5'-cytidylic acid usually adopts the method of microbial synthesis. Although it has a certain scale, the yield is only about 85%, and the quality of the product is not stable. The ultraviolet content is about 97%, and the HPLC content is about Around 97.5%. Contents of the invention [0003] The technical problem to be solved by the present invention is: to overcome the defic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10C07H1/02
Inventor 刘拥军丁楠张剑
Owner NANTONG SANE BIOLOGICAL
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