Tetrahydrofuran substituted uracil compound for treating liver cancer as well as pharmaceutical composition and application thereof

A technology for the treatment of liver cancer with tetrahydrofuran, applied in the field of medicine, can solve the problem of prolongation of less than 3 months

Inactive Publication Date: 2018-11-20
RIZHAO PUDA PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sorafenib is currently the only small-molecule targeted therapy drug for the treatment of liver cancer on the market, with anti-angiogenic therapy as the main mechanism. The extension of the value is less than 3 months, and studies have shown that such molecular targeted drugs ha...

Method used

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  • Tetrahydrofuran substituted uracil compound for treating liver cancer as well as pharmaceutical composition and application thereof
  • Tetrahydrofuran substituted uracil compound for treating liver cancer as well as pharmaceutical composition and application thereof
  • Tetrahydrofuran substituted uracil compound for treating liver cancer as well as pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Synthesis of 1-[(3-methyl)tetrahydrofuran-2-yl]-5-fluorouracil.

[0064]

[0065] The synthesis steps are:

[0066] ;

[0067] First, methanol (550g) was placed in a low-temperature constant temperature reaction bath, and hydrogen chloride gas was added to increase the weight to (600g) to stop ventilation, and a methanol solution of hydrochloric acid was prepared as an acidifying agent;

[0068] Next, add 2-methoxy-5-fluorouracil (compound B) (45g) into the solution containing the acidifier and stir, heat it in a water bath to 35°C and keep it warm for 6 hours. The HPLC monitors the end of the reaction and cools down after the end of the reaction. to 15°C, and suction filtered to obtain 5-fluorouracil (compound C) (40.57 g). After suction filtration, the solution was concentrated to recover methanol;

[0069] Finally, under nitrogen protection, 5-fluorouracil (compound C) (40.57g) was added to 3-methyltetrahydrofuran (compound D) (42g), carbon tetrabromide (80ml)...

Embodiment 2

[0071] Synthesis of 1-[[3-(1-chloroisopropyl-2-yl)]tetrahydrofuran-2-yl]-5-fluorouracil.

[0072]

[0073] The synthesis steps are:

[0074] ;

[0075] First, methanol (600g) was placed in a low-temperature constant temperature reaction bath, and hydrogen chloride gas was introduced to increase the weight to (650g) to stop ventilation, and a methanol solution of hydrochloric acid was prepared as an acidifying agent;

[0076] Next, add 2-methoxy-5-fluorouracil (Compound B) (50g) into the solution containing the acidifier and stir, heat it in a water bath to 30°C and keep it warm for 5 hours. HPLC monitors the end of the reaction, and cools down after the end of the reaction To 15°C, filter with suction to obtain 5-fluorouracil (compound C) (46.78g), and concentrate the solution to recover methanol after suction filtration;

[0077] Finally, under nitrogen protection, 5-fluorouracil (compound C) (46.78g) was added to 3-(1-chloroisopropyl) tetrahydrofuran (compound D) (48....

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PUM

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Abstract

The invention provides a tetrahydrofuran substituted uracil compound for treating liver cancer as well as a pharmaceutical composition and application thereof. The tetrahydrofuran substituted uracil compound has a following chemical structure shown as a formula A. The structural formula is as shown in the description. The tetrahydrofuran substituted uracil compound disclosed by the invention has high inhibitory activity, is capable of interfering synthesis of tumor cell DNA and proteins thereof in vivo so as to inhibit tumor formation and growth of the liver cancer, and can further obviously inhibit pulmonary metastasis and intrahepatic dissemination of the liver cancer.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular, the invention relates to a tetrahydrofuran substituted uracil compound for treating liver cancer and its pharmaceutical composition and application. Background technique [0002] Malignant tumor (cancer) is a major human disease, and it is of great significance to strengthen the research and development of new anti-tumor drugs. There are more than 22 million patients with malignant tumors in the world, 10.1 million new patients are diagnosed every year, and more than 6.2 million patients die of cancer every year. There are at least 3 to 4 million malignant tumor patients in my country, with more than 1.6 million newly diagnosed patients and more than 1.3 million annual deaths. With the rapid development of my country's economy and society, the extension of average life expectancy, and the changes in dietary structure and environmental factors, the incidence and mortality of tumor...

Claims

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Application Information

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IPC IPC(8): C07D405/04A61P35/00A61P35/04A61P1/16A61K31/513
CPCA61P1/16A61P35/00A61P35/04C07D405/04
Inventor 不公告发明人
Owner RIZHAO PUDA PHARMA TECH CO LTD
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