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A compound with quinolinone tetravalent platinum structure, preparation method and application thereof in the preparation of antitumor drugs

A compound, tetravalent platinum technology, applied in the direction of antineoplastic drugs, platinum-based organic compounds, platinum-group organic compounds, etc., can solve problems such as low absorption rate, strong toxic and side effects, and serious drug resistance

Active Publication Date: 2021-06-15
LIAOCHENG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the widespread use of platinum-based drugs in clinical treatment, the disadvantages of strong toxic and side effects, low absorption rate, low bioavailability, poor targeting, and serious drug resistance have gradually emerged, which have seriously affected the clinical application and treatment of platinum-based drugs. Effect

Method used

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  • A compound with quinolinone tetravalent platinum structure, preparation method and application thereof in the preparation of antitumor drugs
  • A compound with quinolinone tetravalent platinum structure, preparation method and application thereof in the preparation of antitumor drugs
  • A compound with quinolinone tetravalent platinum structure, preparation method and application thereof in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
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preparation example Construction

[0063] The preparation method of the above compound is as follows:

[0064] (1) The reaction formula of the asymmetric monoquoquinolinone tetramiplatin compound 1 of the formula 1 is as follows:

[0065]

[0066] Among them, the compound molar ratio of Compound 4, Compound 5, TBTU, and Triethylamine is 1: (1.0-1.3): (1.0-1.3): The relationship between compound 4 and DMF is 1 g: (30) -80ml);

[0067] (2) The reaction type of the symmetric double-substituted quinolinone tetramiplatin compound 2 is as follows:

[0068]

[0069] Among them, the compound molar ratio of Compound 4a, Compound 5, TBTU, and Triethylamine is 1: (2.2 ~ 3): (2.2 to 3): (2.2 to 3), the relationship between compound 4 and DMF is 1 g: (30 ~ 80ml).

[0070] Further, the method of preparing a non-symmetric monoquoquinolinone tetramic platinum compound is as follows:

[0071] The TBTU and quinolinone derivative 5 were added to the reaction vessel, and the air in a nitrogen gas changing system was added, and the...

Embodiment 1

[0091] Example 1: Preparation of quinolinone tetramiplatin compounds shown in Formulas 1 and 2

[0092] 1. Synthesis of dihydroxy-dioxin (IV) 4A-1

[0093]

[0094] To 250 ml round bottom flask, cisplatin 1.0 g, 30 mL of distilled water, stirred, and slowly add concentration of 30% hydrogen oxygen to 50 ml of a concentration of 30%, and the temperature to 60 ° C was stirred in the reaction system. The reaction was stopped, and the crystalline was placed in -4 ° C for 12 hours, the filtration was separated to obtain a yellow solid, adding an appropriate amount of distilled water, heating to 80 ° C, adding 4 ° C for 12 hours, filtered the compound 4A-1 yellow crystal (0.82g 74%).

[0095] 2. Synthesis of Hydroxychloro Osulatin (IV) 4A-2

[0096]

[0097] To the 250 ml round bottom flask, Osli platinum 1.0 g, distilled water was 30 mL, stirred, and the concentration was slowly added dropwise to 50 ml of hydrogen peroxide at a reaction system, and the temperature to 60 ° C was sti...

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Abstract

The invention proposes a compound with a quinolinone tetravalent platinum structure, a preparation method and its application in the preparation of antitumor drugs. The structural formula of the compound is: or The compound has excellent anticancer and antitumor effects.

Description

Technical field [0001] The invention belongs to inorganic chemistry, organic chemistry, and pharmaceutical chemistry, in particular, compounds, preparation methods having quinolinone tetravalent platinum structures, and their applications in the preparation of anti-tumor drugs. Background technique [0002] Cancer is also called malignant tumors, which makes great threats to human life and health. Cancer demonstrates the growth, differentiation and proliferation of body cells that cannot be controlled, and have the characteristics of metastasis and infiltration. With the advancement and development of human society, there is more and more carcinogenic factors, but until today, human beings have failed to completely overcome cancer, so R & D new anti-cancer drugs and creating new medical methods have become many medical research workers. solved problem. [0003] Platinum drugs are the most successful metal anticancer drug in human history, showing broad-spectrum, high-efficiency a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/282A61P35/00
CPCA61P35/00C07F15/0093
Inventor 王庆鹏刘治芳李大成李国帅
Owner LIAOCHENG UNIV