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Oxalic adefovir dipivoxil, and crystalline form and preparing method and use thereof

A technology of adefovir dipivoxil and fovir dipivoxil, which is applied in the field of medicine, can solve problems not involving adefovir dipivoxil, etc., and achieve the effects of easy preparation, good fluidity, and easy purification

Inactive Publication Date: 2004-09-15
HARBIN PHARMA GRP CO LTD GENERAL PHARMA FACTORY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

None of the above three patents involved adefovir dipivoxil

Method used

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  • Oxalic adefovir dipivoxil, and crystalline form and preparing method and use thereof
  • Oxalic adefovir dipivoxil, and crystalline form and preparing method and use thereof
  • Oxalic adefovir dipivoxil, and crystalline form and preparing method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The preparation of embodiment 1 adefovir dipivoxil oxalate crystal form

[0023] Add 10g of adefovir dipivoxil oil to 50mL of acetone, stir at room temperature to dissolve, add dropwise 1.8g of oxalic acid in 20mL of acetone solution, complete, stir at room temperature, and slowly precipitate a white crystalline solid, and place it overnight at 0-5°C. Suction filtration, wash with acetone until neutral, and dry to obtain 10.6 g of adefovir disoproxil oxalate as an off-white powder with a yield of 90%.

[0024] Melting point: 173~175℃

[0025] DSC: 175°C

[0026] Elemental analysis:

[0027] Found C 44.73%, H 5.79%, N 11.64

[0028] Theoretical value (C 20 h 32 N 5 o 8 P.C. 2 o 4 h 2 ) C 44.67%, H 5.75%, N 11.84

[0029] Properties of the crystal form of adefovir disoproxil oxalate

[0030] (1) Infrared absorption spectrum (attached figure 1 )

[0031] At 3090, 2975, 1754, 1697, 1516, 1480, 1461, 1414, 1271, 1228, 1137, 1056, 1027, 969, 888, 706cm -1

[0...

Embodiment 2

[0049] The preparation of embodiment 2 adefovir dipivoxil oxalate crystal form

[0050] Methanol was used to replace the acetone in Example 1, and the others were the same as in Example 1 to obtain adefovir dipivoxil with a yield of 80%.

Embodiment 3

[0051] The preparation of embodiment 3 adefovir dipivoxil oxalate crystal form

[0052] Acetonitrile was used instead of acetone in Experimental Example 1, and the others were the same as in Example 1 to obtain adefovir dipivoxil with a yield of 85%.

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Abstract

The invention is an oxalic acid adefovir dipivoxil and its crystal form as well as preparing method and usage, having stable property and good fluidity, easy to purify and convenient to operate. It is chemically called oxalic acid 9-[2-[bis(pivaloyloxymethoxy)phosphorylmethoxyl]ethyl] adenine. The infrared absorption spectrum measured by KBr sheet has absorption peaks at about 3090, 2975, 1754, 1697 and 1597 cm-1; X-ray powder diffraction spectrum radiated by Cu-Ka and expressed by 20 degrees has characteristic peaks at about 3.9, 15.6, 19.6, 23.6 and 27.5. It is applied to industrialized production and widely applied to prepare the drug of curing virus hepatitis.

Description

Technical field: [0001] The present invention relates to the technical field of medicine, specifically it is oxalic acid 9-[2-[[two (pivaloyloxy) methoxy] phosphinyl] methoxy] ethyl] adenine represented by formula I ( (referred to as adefovir dipivoxil) and its crystal forms as well as their preparation methods and uses. In addition, the present invention also relates to their use as active ingredients in the preparation of medicines for treating viral hepatitis and pharmaceutical compositions containing them. [0002] Background technique: [0003] Adefovir dipivoxil has broad-spectrum antiviral effects against retroviruses, hepadnaviruses, and herpesviruses, and also has immunomodulatory effects. In the preparation of adefovir dipivoxil, its oily substance is usually prepared, which is unfavorable for production, storage and application as medicine. [0004] CN125182A provides four crystal forms of adefovir dipivoxil, and provides some crystalline salts of adefovir di...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K31/675A61P1/16A61P31/12C07F9/6561
Inventor 宫平
Owner HARBIN PHARMA GRP CO LTD GENERAL PHARMA FACTORY
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