Method for preparing intermediate of Entecavir antiviral agent

An inert gas and compound technology, applied in the field of preparation of antiviral drug entecavir intermediates, can solve the problems of expensive raw material reagents, low yield of entecavir intermediates, and unsuitability for industrial production, and achieve low cost and simple reaction conditions , The effect of cheap raw materials

Inactive Publication Date: 2010-12-08
HANDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The purpose of the present invention is to provide a preparation method of an entecavir intermediate, which solves the problems of low yield of entecavir intermediate in the prior art, high cost, expensive raw material reagents, and unsuitability for industrialized production.

Method used

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  • Method for preparing intermediate of Entecavir antiviral agent
  • Method for preparing intermediate of Entecavir antiviral agent
  • Method for preparing intermediate of Entecavir antiviral agent

Examples

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Embodiment 1

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Abstract

The invention discloses a method for preparing an intermediate (I) of an Entecavir antiviral agent, which comprises the following steps: (1) reacting a compound of a formula (II) with magnesium under a condition of a proper solvent to generate a compound of a formula (III); and performing the Grignard reaction of the compound of the formula (III) and a compound of a formula (IV). In the formulae, X and Y are identical or different and may be F, Cl and Br atoms. The method has the advantages of simple reaction conditions, cheap and readily available raw materials, simple and safe process, low cost and easy industrial production.

Description

technical field The invention belongs to the field of pharmaceutical technology, and in particular relates to a preparation method of an antiviral drug entecavir intermediate. Background technique Chronic hepatitis B is a chronic inflammatory necrotic disease of the liver caused by persistent hepatitis B virus (HBV) infection. Fatigue, general malaise, loss of appetite, discomfort or pain in the liver area, abdominal distension, insomnia, low-grade fever, etc. appear clinically. The disease is a common disease that seriously endangers human health. The prevention and treatment of chronic hepatitis B is a global public health problem, which has attracted the attention of countries all over the world. my country is a high incidence area of ​​viral hepatitis, with an average annual incidence rate of 120-140 / 100,000. Among them, hepatitis B (HB) is the most prominent. The infection rate of hepatitis B virus (HBV) in my country is as high as 57.63%, that is, at least 600 milli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F7/12
Inventor 方洋李晨曦殷飞
Owner HANDE PHARMA
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