Prepn process of Adefovir dipivalate

A technology of dipentapentyl ester and trimethylchlorosilane, which is applied in the field of preparing nucleotide analogs 9-[methoxy]phosphinyl]methoxy)ethyl]adenine, can solve the problem of expensive, Problems such as high preparation cost and difficulty in purchasing can achieve the effect of reducing production cost and not affecting product quality and yield

Inactive Publication Date: 2004-06-23
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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  • Abstract
  • Description
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Problems solved by technology

Due to the high price of trimethylbromosilane (about 1480 yuan per 100 grams), the preparation cost is high; and at present, there is no m

Method used

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  • Prepn process of Adefovir dipivalate
  • Prepn process of Adefovir dipivalate
  • Prepn process of Adefovir dipivalate

Examples

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Embodiment 1

[0019] The specific operations of steps A and B are as described in published patents, and the specific implementation of step C is: in a 1000ml three-necked bottle equipped with a condenser tube and a drying tube, replace the air with nitrogen and drop into 130g, that is, 0.395mol of diethyl PMEA, 350g or 8.54mol acetonitrile, 289g or 1.74mol potassium iodide and 192.5g or 1.77mol trimethylchlorosilane, heated to 55°C under stirring, refluxed for 2 hours, then heated to 75°C and refluxed for 3 hours, sampling test (TLC) . After passing the test, remove acetonitrile to dryness under negative pressure (the temperature in the bottle does not exceed 80°C). Cool to room temperature, add 260ml of water to fully dissolve, then raise the temperature to 55°C, stir and keep warm for 1 hour, cool to room temperature, and neutralize with 20% (W / W) sodium hydroxide solution to pH=3.0--3.5. Heat up to 75°C for 1 hour, cool to 0--3°C for 3 hours, and filter to dryness. Transfer the filter...

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Abstract

The present invention discloses one improved preparation process of Adefovir dipivalate. In the synthesis of the mother compound 9-[2-(phosphinocarboxyl methoxy) ethyl adenine, trimethyl chlorsilane, rather than expensive trimethyl bromosilane, as material and potassium iodide as nucleophilic reagentare used to reduce cost while the product yield and quality is maintained. The production process of the present invention may be used in industrial production.

Description

technical field [0001] The present invention relates to a method for preparing nucleotide analog 9-[(2-[[bis(pivaloyloxy)methoxy]phosphinyl]methoxy)ethyl]adenine, specifically It is an improved method related to the preparation of its parent compound substance 9-[2-(phosphinecarboxymethoxyethyl]adenine. Background technique [0002] Nucleotide analogue 9-[(2-[[bis(pivaloyloxy)methoxy]phosphinyl]methoxy)ethyl]adenine, the common name is adefovir dipipate , the English name adefovirdipivoxil (hereinafter referred to as AD), is the parent compound substance 9-[2-(phosphinecarboxymethoxy)ethyl]adenine (hereinafter referred to as PMEA) dipipivoxil, which has antiviral activity on animals and humans , has a strong inhibitory effect on retrovirus, poxvirus, herpes virus and hepatitis B virus. Clinical trials have shown that short-term oral treatment of chronic hepatitis B can significantly reduce the virus, and combining it with other drugs can enhance the cur...

Claims

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Application Information

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IPC IPC(8): A61P31/12C07F9/6561
Inventor 胡祖耀万国成
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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