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9,10-anthraquinone derivatives, their preparation methods and applications
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An anthraquinone derivative and drug technology, applied in 9 fields, can solve the problems of general action strength, increase activity, etc., and achieve the effect of good anti-HCV activity
Active Publication Date: 2022-03-22
SHANGHAI INST OF PHARMA IND CO LTD +1
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Patent CN200810203112.1 also discloses that emodin methyl ether has a certain inhibitory effect on hepatitis C virus, but the strength of the effect is average, and further structural modification is required to increase the activity
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Embodiment 1
[0038]Dissolve 5mmol emodin in 15mL acetone, add 10mmol potassiumcarbonate and 15mmol chloroacetonitrile, heat up to 45°C for 12 hours, distill off the solvent under reduced pressure, add 15mL water, then extract three times with 15mL ethyl acetate, combine the organic phases, 15mL After washing once with water, the compound 1 was obtained by column chromatography (PE / EA=4 / 1) with a yield of 59%.
[0041] The reaction conditions and operations were the same as in Example 1, except that chloroacetonitrile was replaced by ethyl bromoacetate to obtain compound 2 with a yield of 45%.
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Abstract
The invention discloses a 9,10-anthraquinone derivative, its preparation method and application. The present invention provides the application of a 9,10-anthraquinone derivative or a pharmaceutically acceptable salt thereof as shown in formula I in the preparation of medicines for treating and / or preventing hepatitis C; wherein, R is R 1 Replaced C 1 ~C 4 Alkyl; all R 1 Independently for ‑COOR 1‑1 , ‑OH, ‑CN, C 1 ~C 4 Alkyl, or, C 1 ~C 4 Alkoxy; all R 1‑1 independently for C 1 ~C 4 alkyl. The 9,10-anthraquinone derivatives provided by the invention show better anti-HCV activity.
Description
technical field [0001] The invention relates to a 9,10-anthraquinone derivative, its preparation method and application. Background technique [0002] Hepatitis C is caused by hepatitis C virus (HCV) infection and is mainly transmitted by blood / body fluids. The World Health Organization estimates that 170 million people are infected with HCV worldwide. The anti-HCV positive rate of healthy people in my country is 0.7% to 3.1%, about 38 million people. Due to various factors such as the biological characteristics of the virus and the immune function of the host, it is often difficult for the body’s immunity to effectively clear the virus, resulting in about 50% to 80% of HCV-infected patients developing chronic hepatitis, of which 20% to 30% will develop into liver cirrhosis. Every year, 1% to 4% of patients with liver cirrhosis develop hepatocellular carcinoma. Because HCV is transmitted through blood, it is chronic and occult. Some HCV-infected patients will develop chro...
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