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Nucleotide analogue composition and preparing method

A technology of compositions and analogs, applied in the directions of drug combinations, steroids, pharmaceutical formulations, etc., can solve the problems of easy moisture absorption, low melting point, no hepatoprotective and liver protection effects, etc., and achieves low moisture absorption, high melting point, solid good stability

Inactive Publication Date: 2003-06-25
李志海
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For the infection treatment and prevention of various viruses, see WO9904774, CN1264387A, CN1347695A, these substances can react with organic or inorganic acids to form various compositions with different properties, as can be seen from the published literature, these substances It is mainly used for the treatment and prevention of viral infection, but has no hepatoprotective and hepatoprotective effects. For patients with viral infection, both antiviral treatment and hepatoprotective treatment are often needed. Therefore, patients need to take both Functional drugs, and these drugs also have low melting point, easy to absorb moisture, and poor solid state stability. Therefore, developing a new type of composition, adding new varieties, perfecting and improving its various properties is a key issue in our pharmaceutical industry. top priority

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Take 9-[2-[[bis(pivaloyloxy)methoxy]phosphono]methoxy]ethyl]adenine 1.5g (0.0029mol) and dissolve it in 5ml isopropyl at 35°C Alcohol, take 1.365g (0.0029mol) of oleanolic acid and add 17ml of chloroform, heat to dissolve, and 9-[2-[[bis(pivaloyloxy)methoxy]phosphono]methoxy]ethyl ] Slowly add the isopropanol solution of adenine into the chloroform solution, stir for 15 minutes, evaporate the solvent under reduced pressure at 40-50°C, take out the residue, and dry to constant weight at ≤50°C under a 30mmHg column to obtain 9 -[2-[[bis(pivaloyloxy)methoxy]phosphono]methoxy]ethyl]adenine oleanate (codenamed AD oleanate).

[0018] It is consistent with the hypothetical structural formula through elemental analysis, infrared, and NMR spectrum.

[0019] Melting point: not detected

[0020] Elemental analysis: theoretical value C 62.67 H 8.35 N 7.33

[0021] Found C 62.72 H 8.39 N 7.28

Embodiment 2

[0022] Embodiment 2: Get 1.5g (0.0028mol) of 9-[2-(R)-[[bis[[oxycarbonyl]oxyl]methoxy]phosphono]methoxy]propyl]adenine 5ml of isopropanol, take 1.32g (0.0028mol) of oleanolic acid and add 17ml of chloroform, heat to dissolve, and dissolve 9-[2-(R)-[[bis[[oxycarbonyl]oxy]methoxy] Slowly add the isopropanol solution of phosphono]methoxy]propyl]adenine into the chloroform solution, stir for 15 minutes, distill off the solvent at 30-40°C under reduced pressure, take out the residue, and store at ≤50°C, 30mmHg column and dry to constant weight at 9°C to obtain 9-[2-(R)-[[bis[[oxycarbonyl]oxy]methoxy]phosphono]methoxy]propyl]adenine oleanolic acid Salt (code-named TD · oleanate).

[0023] It is consistent with the hypothetical structural formula through elemental analysis, infrared, and NMR spectrum.

[0024] Melting point: not determined.

[0025] Elemental analysis: theoretical value C 60.28 H 8.05 N 7.18

[0026] Found C 60.21 H 8.01 N 7.16

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PUM

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Abstract

The present invention provides the oleanolate of phosphono methoxy nucleotide analogue composition and its preparation process. The composition is used in preventing and treating viral diseases and hepatitis. The composition has the functions of both resisting virus and protecting liver and has high smelting point, low hygroscopicity, high stability and high yield in synthesis process, and may be prepared in large scale.

Description

(1) Technical field: [0001] The present invention relates to a class of compounds capable of treating and preventing viral diseases and hepatitis, in particular to a nucleotide analog composition and preparation method (two) background technology: [0002] Phosphonomethoxy nucleotide analogs are known substances. For the infection treatment and prevention of various viruses, see WO9904774, CN1264387A, CN1347695A, these substances can react with organic or inorganic acids to form various compositions with different properties, as can be seen from the published literature, these substances It is mainly used for the treatment and prevention of viral infection, but has no hepatoprotective and hepatoprotective effects. For patients with viral infection, both antiviral treatment and hepatoprotective treatment are often needed. Therefore, patients need to take both Functional drugs, and these drugs also have low melting point, easy to absorb moisture, and poor solid state stabilit...

Claims

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Application Information

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IPC IPC(8): A61K31/7076A61P1/16A61P31/12C07J63/00
Inventor 李志海
Owner 李志海
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