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Nucleoside phosphate and synthesis method thereof

A technology of nucleoside phosphate ester and synthesis method, which is applied in the field of preparation of nucleoside phosphate ester, can solve problems such as easy occurrence of fire and explosion, and achieve the effects of avoiding fire or explosion, avoiding cumbersome operations and avoiding corrosion

Active Publication Date: 2021-01-29
南京颐媛生物医学研究院有限公司 +1
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Problems solved by technology

[0009] , the method adopts simple operation to synthesize phosphoric acid diester triethylamine salt, greatly simplifies post-processing operation, but this method needs to use hydrogen and Pd / C catalyst to carry out catalysis in the process of synthesizing phosphoric acid diester triethylamine salt Debenzylation, prone to fire or even explosion hazard [WO 2015 / 200205 A1]

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  • Nucleoside phosphate and synthesis method thereof
  • Nucleoside phosphate and synthesis method thereof
  • Nucleoside phosphate and synthesis method thereof

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Embodiment Construction

[0038] Specific embodiments of the present invention are described in detail below, but it should be understood that the protection scope of the present invention is not limited by the specific embodiments.

[0039] Unless expressly stated otherwise, throughout the specification and claims, the term "comprise" or variations thereof such as "includes" or "includes" and the like will be understood to include the stated elements or constituents, and not Other elements or other components are not excluded.

[0040] Wherein the raw material phosphoric acid diester lithium salt is synthesized according to the following route:

[0041] ,

[0042] The first step of the route follows the literature [Yousang, Hwang.; Philip A. Cole. org. Lett. 2004, 6, 1555.] The method introduced, the second step of the route is in accordance with [Kim C. Calvo.; Xiaohong Wang.; Gerald F.Koser. Nucleos. Nucleot. Nucl. 2004, 23, 637.] The method introduced.

[0043] D / L-2', the synthesis of nuc...

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Abstract

The invention discloses a synthesis method of nucleoside phosphate, which mainly comprises the following steps: mixing lithium diphosphate, nucleoside and a condensing agent in a solvent, stirring atroom temperature, adding a citric acid solution for washing after the reaction is finished, drying with anhydrous sodium sulfate to obtain a crude product, and carrying out column chromatography separation to obtain the product. According to the method disclosed by the invention, ion exchange resin does not need to be used for treatment in the process of synthesizing the raw material phosphodiester, the reaction can be carried out by directly using the lithium diphosphate, the method disclosed by the invention is simple to operate and low in equipment requirement, and the same meaningful method is provided for synthesizing nucleoside diphosphate.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a preparation method of nucleoside phosphate. Background technique [0002] Resistance to nucleosides sometimes results from loss or reduced activity of the major kinases that convert nucleosides to the corresponding nucleoside-5'-monophosphate. This resistance mechanism cannot be overcome by direct use of nucleoside-5'-nucleoside monophosphates, as these compounds do not penetrate cells efficiently and are usually rapidly dephosphorylated to nucleosides by extracellular phosphatases. In order to overcome this deficiency, Saeed R. Khan et al. developed a method for attaching a phosphodiester at the 5' position of the nucleoside. [US Patent 4,816,570 (1989)] By introducing nucleoside-5'-position hydroxyl into phosphodiester, nucleoside compounds can enter the cell by passive diffusion, so the synthesis of nucleoside phosphodiester has attracted the attenti...

Claims

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Application Information

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IPC IPC(8): C07H1/00C07H19/207C07H19/10
CPCC07H1/00C07H19/10C07H19/207Y02P20/55
Inventor 袁仁涛鲍甫义马丁来冯力佟有恩李小波周明
Owner 南京颐媛生物医学研究院有限公司
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