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Diethylcarbamyl-substituted thiazole dihydropyrimidine

A thiazole and alkyl technology, applied in the field of ethoxycarbonyl-substituted thiazole dihydropyrimidines, can solve problems such as side reactions and rebound effects

Active Publication Date: 2008-12-24
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, interferons are only moderately active and have deleterious side effects; while lamivudine has good activity, resistance develops rapidly during treatment and rebound effects often occur after cessation of treatment

Method used

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  • Diethylcarbamyl-substituted thiazole dihydropyrimidine
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Ethyl 4-(2-chloro-4-fluorophenyl)-2-(thiazol-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate

[0134]

[0135] 10.0g (63.1mmol) of2-chloro-4-fluorobenzaldehyde, 8.2g (63.1mmol) ethylacetoacetic acid, 10.3g (63.1mmol) 2-amidino-thiazole hydrochloride and 6.2g (75.7mmol) acetic acid Sodium was dissolved or suspended in 500ml of ethanol and boiled under reflux for 16 hours. Cool to room temperature, filter with suction, and wash the residue with water to remove inorganic salts. 12.8 g (53.4%) of product were obtained, melting point: 162-164°C.

Embodiment 2

[0137] Methyl 4-(2-chloro-4fluorophenyl)-2-(thiazol-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate This compound uses methyl acetoacetate Synthesized according to the method similar to Example 1.

[0138] Yield: 55% (melting point: 152-154°C)

Embodiment 3

[0140] Ethyl 4-(2-bromo-4fluorophenyl)-2-(thiazol-2-yl)-6-methyl-1,4-dihydropyrimidine-5-carboxylate This compound uses ethyl acetoacetate Synthesized according to the method similar to Example 1.

[0141] Yield: 51.6% (melting point: 163-165°C)

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Abstract

The invention relates to a sulphoxide and sulphone containing novel thiazolyldihydropyrimidine applicable to acting against hepatitis B virus (HBV) infection and a composition of the same and other antiviral agents.

Description

technical field [0001] The present invention relates to a new ethoxycarbonyl-substituted thiazole dihydropyrimidine, its preparation method and its use as medicine, especially its application in treating and preventing hepatitis B virus infection. The present invention also relates to the composition of these dihydropyrimidines with other antiviral agents and, where appropriate, immunomodulators, and medicaments containing these compositions, especially for the treatment and prevention of HBV infection, such as hepatitis B. Background technique [0002] Hepatitis B virus belongs to the Hepaviridae family. It can cause acute and or persistent / progressive chronic disease. Hepatitis B virus also causes many other clinical signs in the pathomorphology - notably chronic inflammation of the liver, cirrhosis and carcinogenesis of hepatocellular cells. In addition, co-infection with hepatitis D can have detrimental effects during the development of the disease. [0003] Conventio...

Claims

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Application Information

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IPC IPC(8): C07D417/04A61K31/541A61K31/445A61P31/12A61P1/16
CPCA61P1/16A61P31/12C07D401/04C07D401/14C07D417/04C07D417/14
Inventor S·戈尔德曼李静刘遗松
Owner SUNSHINE LAKE PHARM CO LTD
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