Process for preparation of nucleoside phosphoric acid ester compound and application thereof

A nucleoside phosphate and compound technology, applied in the field of nucleoside phosphate compounds, can solve the problems of being unable to be transformed, showing no biological activity, etc.

Inactive Publication Date: 2008-01-23
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For some polar compounds, nucleoside 5'-monophosphate is difficult to enter the cell and cannot be converted into its biologically active 5'-triphosphate, so it has no biological activity

Method used

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  • Process for preparation of nucleoside phosphoric acid ester compound and application thereof
  • Process for preparation of nucleoside phosphoric acid ester compound and application thereof
  • Process for preparation of nucleoside phosphoric acid ester compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0037] 1. Preparation of compound 4:

[0038] a. Compound 3 was prepared from uridine according to the method patented by (Clark, J. PTC Patent Appl. WO 2005 / 003147).

[0039]

[0040] b. Preparation of phosphodiester:

[0041] At 0°C, POCl 3 (4mmol) was added dropwise to the solution containing phenol (4mmol) and Et 3 N (4 mmol) in diethyl ether solution, then the reaction mixture was stirred overnight at room temperature, the solid salt was removed by filtration, and the filtrate was evaporated to dryness to obtain crude dichlorophosphate 2.

[0042] At 0°C, the above-mentioned dichlorophosphate was added dropwise into a solution of nucleoside 3 (2mmol) in pyridine (10ml), and the reaction mixture was stirred at 0°C and room temperature for 1 hour, then at 100°C for 8 hours, and evaporated under reduced pressure. pyridine, the residue was dissolved in CH 2 Cl 2 (100ml). Washed, Na 2 SO 4 After drying, the solvent was evaporated, and the residue was separated by si...

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Abstract

The invention provides the nucleoside phosphate compound and the preparation and application, which comprises the nucleoside 3', 5'-cyclic phosphate and the 5'-phosphodiester compound. Wherein, the 3', 5'-cyclic phosphate and the derivatives work as the novel HCV inhibitor and the structural formula is shown in the drawing (I), wherein, X equals to OH and F; R equals to H, NH4, R' 4N, R' 3NH and metals such as Na, K, Ca and Li or the structural formula in the drawing (II), R' equals to linear chain or substituted alkane or cyclane, aromatic hydrocarbon, or substituted aromatic hydrocarbon or heterocyclic aromatic hydrocarbon; the four R' and three R' in the amine are the same or different. The invention has the advantages that the nucleoside phosphate compound is used for treating the HCV or is combined with the Alpha-interferon, ribavirin or other anti-HCV drugs to treat the infection of the hepatic c virus or HCV.

Description

technical field [0001] The invention relates to a nucleoside phosphate compound, a preparation method and an application. It belongs to the technical field of nucleoside phosphate compounds. Background technique [0002] In recent years, hepatitis C virus (Hepatitis C Virus, HCV) infection has attracted more and more attention, and the number of HCV carriers is increasing year by year. About 30% of HCV carriers will develop chronic hepatitis, and about 20% of their chronic hepatitis C patients may develop liver cancer. However, so far, the drug used to treat hepatitis C virus infection is only a so-called standard therapy, namely alpha-interferon or a combination of alpha-interferon and ribavirin. Taking no recurrence 6 months after stopping the drug as the standard, the effective rate is only 40%, and some patients will give up treatment because of the side effects of the drug. Therefore, new drugs are urgently needed to meet the needs of patients. [0003] Over the pas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/10A61K31/7068A61P1/16A61P31/12
Inventor 冷一欣
Owner 冷一欣
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