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Adefovir dipivoxil new crystal state, new crystal state composition and its preparing method

A technology of adefovir dipivoxil and composition, applied in the field of new crystal state of nucleoside drugs, new crystal state composition and preparation thereof, can solve the problems of high cost, harsh conditions, unfavorable large-scale industrial manufacturing and the like, To achieve the effect of no reduction in drug content, easy production and good crystal stability

Inactive Publication Date: 2003-06-25
SUZHOU ERYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The preparation process of the crystalline and amorphous adefovir dipivoxil (W.O 9904774 and C.N1374314) publicly reported is tedious, the conditions are harsh, and the cost is high, which is not conducive to large-scale industrial manufacturing

Method used

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  • Adefovir dipivoxil new crystal state, new crystal state composition and its preparing method
  • Adefovir dipivoxil new crystal state, new crystal state composition and its preparing method
  • Adefovir dipivoxil new crystal state, new crystal state composition and its preparing method

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Embodiment 1 Alcohol method prepares adefovir dipivoxil new crystal state

[0021] Add 50g of adefovir dipivoxil into a 500ml flask, add 200ml of absolute ethanol at 20-30°C to dissolve it, and spin dry the solvent under reduced pressure at 50°C until it becomes a colorless oil, then rapidly heat up to 80 ℃, the oil can quickly expand into a honeycomb. After all the remaining solvents were volatilized, it was then vacuum-dried at 50° C. for 5 hours to obtain a new crystalline form of adefovir dipivoxil with a purity of 90%.

Embodiment 2

[0022] Embodiment 2 ketone method prepares adefovir dipivoxil new crystal state

[0023] Add 50g of adefovir dipivoxil into a 500ml flask, add 300ml of acetone at 20-30°C to dissolve it, spin-dry the solvent under reduced pressure at 30°C until it becomes a colorless oily substance, then rapidly heat up to 60°C, The oil can quickly expand into a honeycomb. After all the residual solvents were volatilized, it was then vacuum-dried at 50° C. for 5 hours to obtain a new crystalline form of adefovir dipivoxil with a purity of 85%.

Embodiment 3

[0024] Embodiment 3 ester method prepares adefovir dipivoxil new crystal state

[0025] Add 50g of adefovir dipivoxil into a 500ml flask, add 400ml of ethyl acetate at 20-30°C to dissolve it, and other operations are the same as in Example 2 to obtain a new crystalline form of adefovir dipivoxil with a purity of 88%. .

[0026] Embodiment 4 halogenated hydrocarbon method prepares adefovir dipivoxil new crystal state

[0027] Add 50g of adefovir dipivoxil into a 500ml flask, add 200ml of chloroform at 20-30°C to dissolve it, and other operations are the same as in Example 2 to obtain a new crystalline form of adefovir dipivoxil with a purity of 88%. .

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Abstract

The present invention describes a new crystal state of adefovir depivoxil and its preparation process as well as the composite of the new crystal state and its preparation process. The new crystal state and the composite are easy to prepare, stable and suitable for industrial production and storage.

Description

technical field [0001] The present invention relates to a new crystal state of nucleoside drugs, a new crystal composition and a preparation method thereof, more specifically to a new crystal state of adefovir dipivoxil, a new crystal composition and its preparation method. Preparation. Background technique [0002] The chemical name of adefovir dipivoxil is 9-{[2-(di-pivaloyloxymethoxy)phosphorylmethoxy]ethyl}adenine. It is a new type of antiviral drug, which can treat human and animal retrovirus infections (such as HIV, SIV, FIV, etc.), various hepatitis virus infections (such as HBV, HCV, etc.) and DNA virus infections (such as Herpes virus, HSV1, HSV2, etc.) showed good antiviral activity. Relevant information disclosures include: U.S. Patent U.S 4724233; European Patent E.P 481214; Starrett et al., Antiviral Res. (1992) 19: 267-273, and J.Med.Chem. (1994) 37: 1857-1864; Benzaria et al., J. Med. Chem. (1996) 39: 4958-4965; Zhang Yong et al., Journal of Shenyang Pharma...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61P31/12C07F9/6561
Inventor 周华明周英王爱明陆飞
Owner SUZHOU ERYE PHARMA CO LTD
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