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Process for preparing purine derivatives

A technology for derivatives and purines, applied in the field of preparing purine derivatives, can solve the problems of unsuitable large-scale preparation of entecavir raw materials, complicated preparation process and the like

Active Publication Date: 2007-08-15
CHIA TAI TIANQING PHARMA GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these preparation processes are relatively complicated, requiring separation and purification conditions that are not suitable for amplification such as column chromatography separation, and are not suitable for industrial large-scale preparation of entecavir raw materials

Method used

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  • Process for preparing purine derivatives
  • Process for preparing purine derivatives
  • Process for preparing purine derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0056] 1) Preparation of Intermediate A

[0057]

[0058] Put 500ml of dry tetrahydrofuran in a 2000ml three-necked flask, and cool it to about -75°C with liquid nitrogen under the protection of nitrogen, and add 116.0g (0.68mol) of 4-methyl-benzylchloromethyl to the reaction flask ether. Put 392ml (0.69mol) cyclopentadiene sodium tetrahydrofuran solution in the balance funnel, then slowly add it dropwise into the reaction flask, control the reaction temperature at -60~-50°C, and continue to stir at this temperature for 1 hours, the intermediate A was directly used in the next reaction.

[0059] 2) Preparation of intermediate (1)

[0060] Preparation of IPC2BH

[0061]

[0062] Draw 800.0 ml (0.80 mol) of borane tetrahydrofuran solution (1.0 mol) with a syringe, and place it in an accurately weighed 250 ml two-necked round bottom flask equipped with a -80°C thermometer and a stirring bar. Under the protection of N2, cool in an ice bath to 0°C, extract 160.0ml (0.902m...

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Abstract

The invention discloses a making method of purine derivant with maleate monohydrate, which also provides drug composition to treat hepatitis B and / or accompanying infection.

Description

field of invention [0001] The present invention relates to a new method for preparing purine derivatives, a pharmaceutical composition containing the compound and its use for treating hepatitis B virus infection and / or concurrent infection. Background technique [0002] [1S-(1α,3α,4β)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H- Purin-6-one (Entecavir, Entecavir) is a new anti-hepatitis B virus drug developed by Bristol-Myers Squibb. It is a purine derivative and has a strong anti-hepatitis B virus effect. Clinically, entecavir is used to treat chronic hepatitis B in adults, including increased hepatitis virus replication activity, elevated transaminase (ATL or AST) in plasma, and active lesions in liver tissue, HBeAg positive or negative with compensated chronic liver disease. Nucleoside-naïve patients with disease, and patients who are resistant to lamivudine. [0003] US Patent Publication No. US5206244 describes entecavir, its prepara...

Claims

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Application Information

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IPC IPC(8): C07D473/18A61K31/522A61P31/12A61P1/16
Inventor 李志兵
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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