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Abacavin preparing process

A technology of amino and methanol, applied in organic chemistry, antiviral agents, etc., can solve problems such as cumbersome processes, achieve the effects of easy-to-obtain raw materials, save steps, and reduce the cost of finished medicines

Inactive Publication Date: 2006-03-01
上海玛耀化学技术有限公司
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

A total of six steps are required from the starting material to the finished product, including diazo, coupling, reduction and other steps, the process is too cumbersome

Method used

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example

[0015] A: Synthesis of [(4-bromo)-cyclopent-2-en-1-yl]methanol

[0016] Add 11.3 grams (0.1 mol) of [(4-amino)-cyclopent-2-en-1-yl]methanol (synthesized according to relevant patents) into a 250 ml four-neck bottle, cool, stir, and slowly add 50 ml 48% hydrobromic acid, cooled to about 0°C. Slowly add 40 grams of aqueous solution made of 6.9 grams (0.1 mole) of sodium nitrite dropwise. Keep the reaction temperature in the bottle at about 0°C, and use starch-potassium iodide test paper to detect the end point of diazotization before the drop is completed. The diazonium reaction solution after the end point was still placed in ice salt.

[0017] In a 500ml four-necked flask equipped with a condenser, a stirrer and a thermometer, 10 grams of cuprous bromide, 20 grams of 48% hydrobromic acid and 0.5 gram of phenothiazine (polymerization inhibition) were added. Heat to near boiling. Under vigorous stirring, the heating was continued, and the above diazotization reaction solutio...

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Abstract

The present invention provides abacavin preparing process. The process includes the reaction between 4-chloro-2-amino-purine and [(4-bromo)-cyclopentyl-2-ene-1-radical] methanol to prepare the key intermediate {(1R, 4S)-4-(2-amino-6-chloro-9H-purine-9 radical) -cyclopentyl-2-ene-1-radical} methanol; and subsequent known process to prepare abacavin. The present invention has less reaction steps, simple operation and easy-to-obtain material, and is suitable for industrial production.

Description

Technical field: [0001] The invention belongs to the technical field of medicinal chemistry. Specifically relates to a method of manufacturing abacavir. Background technique: [0002] Abacavir (ABACAVIR) is a new anti-AIDS (AIDS) drug developed in the United States in recent years. It belongs to the class of nucleoside HIVRT inhibitors. It is used for retroviruses and has excellent therapeutic effects. [0003] AIDS is extremely harmful to human beings, and the development trend is extremely serious. It is imperative to replace the more primitive drugs with new drugs, increase the efficacy of drugs, and effectively curb the spread of the disease. After years of hard research, Glaxo Corporation of the United States has developed a new generation of anti-AIDS (AIDS) nucleoside drug - Abacavir (ABACAVIR), and has registered a patent internationally. The patent number is US5034394. The original process route is as follows : [0004] [0005] [0006] [0007] The sta...

Claims

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Application Information

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IPC IPC(8): C07D473/16C07D473/40A61P31/18
Inventor 孙猛黄强陈品岗
Owner 上海玛耀化学技术有限公司
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