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Crystal structure for medicinal compound adefovir divoxil, and its preparing method and medicine

A technology of adefovir dipivoxil and crystal structure, applied in the field of nucleoside medicinal compounds, can solve the problems of high solvent toxicity, high cost of preparation of adefovir dipivoxil crystal form, unfavorable environmental protection, etc.

Inactive Publication Date: 2005-02-16
四川倍达尔新技术开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The preparation cost of the adefovir dipivoxil crystal form reported in the above literature is high, the yield is low, it is not conducive to large-scale industrial production, and some solvents are highly toxic, which is not conducive to environmental protection

Method used

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  • Crystal structure for medicinal compound adefovir divoxil, and its preparing method and medicine
  • Crystal structure for medicinal compound adefovir divoxil, and its preparing method and medicine
  • Crystal structure for medicinal compound adefovir divoxil, and its preparing method and medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The preparation method one of embodiment 1 adefovir dipivoxil crystal

[0034] Take raw material adefovir dipivoxil crude product 31.0g, add 650ml of isopropyl acetate to dissolve, transfer the solution to a 2L separatory funnel, wash twice with 100ml×2 saturated saline, separate the liquids, add anhydrous sulfuric acid to the organic layer Dry magnesium, filter, concentrate to dryness under reduced pressure at 50°C, add 100ml of acetone to dissolve the solid, filter to remove insoluble matter, transfer the filtrate to a 250ml round bottom flask, heat at 60°C to reflux for 1h, and pour into 1000ml of ice-cold iso In propyl ether, stirring vigorously at the same time, a solid was precipitated, washed with cold isopropyl ether, and the filter cake was vacuum-dried at room temperature to constant weight to obtain 25.5 g of adefovir dipivoxil new crystal form, yield: 82%, content ≥ 99 % (HPLC). The X-ray powder diffraction spectrum, DSC collection of illustrative plates an...

Embodiment 2

[0035] Example 2 Preparation method two of the new crystal form of adefovir dipivoxil

[0036]Take 50.0 g of the raw material adefovir dipivoxil crude product, add 1000 ml of ethyl acetate to dissolve, transfer the solution to a 5 L separatory funnel, wash with 300 ml × 3 saturated saline three times, separate the layers, and dry the organic layer with anhydrous magnesium sulfate , filtered, concentrated to dryness under reduced pressure at 50°C, dissolved the solid with 300ml acetone, filtered to remove insoluble matter, transferred the filtrate to a 500ml round bottom flask, heated to reflux at 60°C for 1h, and poured into 1000ml ice-cold butyl ether while heating , while stirring vigorously, a solid was precipitated, washed with cold butyl ether, and the filter cake was vacuum-dried to constant weight at room temperature to obtain 42.5 g of adefovir dipivoxil new crystal form, yield: 85%, content ≥ 99% (HPLC) . The X-ray powder diffraction spectrum, DSC collection of illus...

Embodiment 3

[0037] Embodiment 3 Preparation method three of adefovir dipivoxil crystals

[0038] Take 62.0g of adefovir dipivoxil crude product, add 1000ml of ethyl acetate to dissolve, transfer the solution to a 5L separatory funnel, wash twice with 300ml×2 saturated saline, separate the layers, and dry the organic layer with anhydrous magnesium sulfate , filtered, concentrated to dryness under reduced pressure at 50°C, dissolved in 300ml of cyclohexanone for the solid, filtered to remove insoluble matter, transferred the filtrate to a 500ml round bottom flask, heated to reflux at 60°C for 1h, poured into 1000ml of ice-cold iso In propyl ether, stirring vigorously at the same time, a solid was precipitated, washed with cold isopropyl ether, and the filter cake was vacuum-dried at room temperature to constant weight to obtain 51.5 g of adefovir dipivoxil new crystal form, yield: 83%, content ≥ 99 % (HPLC). The X-ray powder diffraction spectrum, DSC collection of illustrative plates and I...

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Abstract

The invention is a new crystallographic form of adefuwe ester, a nucleoside officinal medicine, its preparation method and a medicine, which chooses the adefuwe ester as the effective drug ingredients, used to cure the virus hepatitis.

Description

technical field [0001] The present invention relates to a new crystal form of a nucleoside medicinal compound—Adefovir dipivoxil (Adefovir Dipivoxil) and a preparation method thereof, and a drug prepared with the crystal structure of Adefovir dipivoxil as an active pharmaceutical ingredient that can be used for Medicines to treat viral hepatitis. Background technique [0002] The chemical name of Adefovir Dipivoxil is 9-{2-[bis(pivaloyloxymethoxy)phosphorylmethoxy]ethyl}adenine, which is a nucleoside antiviral drug The compound can be rapidly hydrolyzed into adefovir after oral administration to exert antiviral effect. The compound can inhibit the activity of HBV viral DNA polymerase, and can be incorporated into the viral DNA chain to terminate the extension of the viral DNA chain, so it has a significant inhibitory effect on the hepatitis virus. At the same time, it also has a significant therapeutic effect on drug-resistant HBV strains such as lamivudine and other nucle...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61P1/16A61P31/12C07F9/6561
Inventor 黄衡邓兰
Owner 四川倍达尔新技术开发有限公司
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