High-activity jateorhizine platinum (II) complex and synthesis method and application thereof

A synthesis method and jatrorrhizine technology, applied in the field of platinum-based highly active complexes and synthesis, can solve problems such as metal complexes that have never existed before, achieve superior in vivo and in vitro anti-tumor activity and targeting, mild reaction conditions, and synthetic routes simple effect

Active Publication Date: 2019-07-26
YULIN NORMAL UNIVERSITY
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  • Abstract
  • Description
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Problems solved by technology

Judging from the current reports, there has never b

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  • High-activity jateorhizine platinum (II) complex and synthesis method and application thereof
  • High-activity jateorhizine platinum (II) complex and synthesis method and application thereof
  • High-activity jateorhizine platinum (II) complex and synthesis method and application thereof

Examples

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Example Embodiment

[0047] Example 1

[0048] In a 50 mL round-bottom flask, weigh 1.0 mol of Derivative 1, 0.8 mol of potassium chloride, and 1.50 mol of dimethylpyridine amine, and dissolve them in 5.0 ml of acetonitrile solution. After reacting at 90°C for 4 hours, A yellow solid powder of Jat1 ligand was obtained with a yield of 86.0%. The reaction temperature is 90°C, the product sticks to the bottom and carbon chain scission occurs when the temperature is higher than 90°C, and the reaction hardly occurs when the temperature is lower than 90°C.

[0049] Weigh 1.0 mol of ligand Jat1 and the equivalent amount of dichloro·bis(dimethylsulfoxide)platinum(II) in a 100.0mL high-pressure bottle, and dissolve them in 10.0mL acetonitrile solution at 60℃ The coordination reaction was carried out for 4.0 h, washed with acetonitrile and dried in vacuum at a temperature of 40° C. to obtain the target product Pt1 in yellow-brown color. The yield was 95.3%.

Example Embodiment

[0050] Example 2

[0051] In a 50 mL round-bottom flask, weigh 1.0 mol of Derivative 2, 0.8 mol of potassium chloride, and 1.50 mol of dimethylpyridine amine, and dissolve them in 5.0 mL of acetonitrile solution. After reacting at 90°C for 4 hours, A yellow solid powder of Jat2 ligand was obtained with a yield of 81.0%.

[0052] Weigh 1.0 mol of ligand Jat2 and the equivalent amount of dichlorobis(dimethylsulfoxide) platinum(II) in a 100.0mL high-pressure bottle, and dissolve them in 5.0mL acetonitrile solution at 60℃ The coordination reaction was carried out for 4.0 h, washed with acetonitrile and dried in vacuum at a temperature of 40° C. to obtain the target product Pt2 in yellow-brown color. The yield was 90.8%.

Example Embodiment

[0053] Example 3

[0054] The difference from Example 1 is that 1.0 mol of the ligand Jat1 and the equivalent amount of dichloro-bis(dimethylsulfoxide) platinum (II) were weighed in a 100.0 mL high pressure bottle, and dissolved In 90.0 mL of acetonitrile solution, the coordination reaction was carried out at 60° C. for 4.0 h, washed with acetonitrile and dried in vacuum at 40° C. to obtain the yellow-brown target product Pt1. The yield was 70.5%.

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Abstract

The invention relates to a high-activity jateorhizine platinum (II) complex and a synthesis method thereof as well as an application of the complex in preparing anti-cancer drugs. The synthesis methodincludes: 1), dissolving brominated jateorhizine derivatives, potassium chloride and dimethyl arsenic amine into a solvent for reaction at 90DEG C to obtain yellow solid powder which is a Jat ligand;2), dissolving the Jat ligand prepared in the step 1) and dichlorodium (dimethyl sulfoxide platinum) (II) in an acetonitrile solution for complexation reaction at 55-65DEG C; 3), washing and drying the product to obtain the target product. In the synthesis method, the novel jateorhizine derivative Jat is firstly taken as the active ligand to be synthesized the platinum complex, superior antitumoractivity and targeting in vitro and in vivo are shown, potential medicinal value is achieved, and the jateorhizine derivative Jat is expected to be used in the preparation of various antitumor drugs.The structural formula of the high-activity jateorhizine platinum (II) is shown as follows.

Description

technical field [0001] The invention relates to a platinum-based high-activity complex and a synthesis method thereof, in particular to a high-activity jatrorrhizine platinum (II) complex and a synthesis method thereof. The invention also relates to the application of the highly active jatrorrhizine platinum (II) complex in the preparation of antitumor drugs. Background technique [0002] According to incomplete statistics, more than six million people die of cancer every year in the world. Cancer has become one of the common and frequently-occurring diseases that seriously affect and threaten human health (Guo, Z.; et al. Chem. Soc. Rev., 2013, 42:202–224.). In order to treat cancer, scientists have made unremitting efforts to synthesize many platinum-based anticancer drugs such as classic cisplatin and its derivatives; however, these cisplatin-based drugs are prone to drug resistance, high toxicity, water-soluble Poor performance restricts their curative effect and use. ...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0093
Inventor 覃其品王振凤黄小玲
Owner YULIN NORMAL UNIVERSITY
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