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Method for preparing lamivudine intermediate

A technology for lamivudine and intermediates, which is applied in the field of preparation of lamivudine intermediates, can solve the problems of difficulty in controlling the purity, low yield of intermediates, high isomer impurities, etc., and achieves cheap and easy-to-purchase Effect

Inactive Publication Date: 2010-12-15
TIANJIN SEGA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The intermediate obtained by this method not only has a low yield, but also has high isomer impurities, and the purity is difficult to control

Method used

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  • Method for preparing lamivudine intermediate

Examples

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Effect test

Embodiment 1

[0016] Example 1 Put 900ml of toluene, 184g of compound (I) and 20g of glacial acetic acid into a dry reaction flask, heat to reflux to separate water, evaporate 600ml of toluene, cool to 80-85°C, add 60.8g of thiane , after 1 hour of heat preservation, after cooling until crystals precipitated, add 800ml of a mixed solution of N,N-dimethylaniline and n-hexane (0.5:100), stir, cool to 0-5°C, keep heat for 8 hours, and filter , dried to obtain 203.1 grams of product, yield 88.2%.

Embodiment 2

[0017] Example 2 Put 900ml of toluene, 184g of compound (I) and 20g of glacial acetic acid into a dry reaction flask, heat to reflux to separate water, evaporate 600ml of toluene, cool to 80-85°C, add 60.8g of thiane , after keeping warm for 1 hour, after cooling until crystals precipitated, add 800ml of a mixed solution of N,N-dimethylaniline and n-hexane (1:100), stir, cool to 0-5°C, keep warm for 8 hours, and filter , dried to obtain 206.2 grams of product, yield 89.5%.

Embodiment 3

[0018] Example 3 Put 900ml of toluene, 184g of compound (I) and 20g of glacial acetic acid into a dry reaction flask, heat to reflux to separate water, evaporate 600ml of toluene, cool to 80-85°C, add 60.8g of thiane , after keeping warm for 1 hour, after cooling until crystals precipitated, add 800ml of a mixed solution of N,N-dimethylaniline and n-hexane (2:100), stir, cool to 0-5°C, keep warm for 8 hours, and filter , dried to obtain 200.2 grams of product, yield 86.9%.

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Abstract

The invention relates to a method for preparing a lamivudine intermediate. The lamivudine intermediate (II) is prepared by reacting a compound (I) with thiane and taking the mixed solution of N,N-dimethylaniline and normal hexane as a chiral auxiliary. The synthesis method for producing the lamivudine intermediate has the advantages of high yield, high purity, easier crystal form control and easy large-scale production.

Description

technical field [0001] What the present invention relates to is a kind of preparation method of lamivudine intermediate. Background technique [0002] Chronic hepatitis B is a potentially fatal disease. According to the World Health Organization, hepatitis B has become the ninth leading cause of death in humans, and more than 90% of liver cirrhosis and liver cancer are caused by hepatitis B. my country is a high-incidence area of ​​hepatitis B in the world, and it is also the largest market for hepatitis B therapeutic drugs. In 2005, the market size exceeded the sum of the markets of the United States, France, Germany, Italy and Spain. According to the "China Health Statistical Yearbook" in 2007, the incidence of viral hepatitis in my country has increased rapidly, from 64.91 / 100,000 in 2000 to 102.09 / 100,000 in 2006, and the number of chronic hepatitis B patients has reached more than 2,000 million people, accounting for about 1.6% of the total population. The hepatitis B ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D327/04
Inventor 吕丙民郑洁
Owner TIANJIN SEGA PHARMA
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