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A kind of jatrorrhizine platinum (ii) complex and its synthesis method and application

A complex and jatrorrhizine technology, which is applied in the field of platinum complexes and synthesis, can solve problems such as metal complexes that have never existed before, and achieve potential medicinal value, mild reaction conditions, and good targeted inhibition effects

Active Publication Date: 2021-09-07
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Judging from the current reports, there has never been a metal complex with jatrorrhizine as a ligand.

Method used

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  • A kind of jatrorrhizine platinum (ii) complex and its synthesis method and application
  • A kind of jatrorrhizine platinum (ii) complex and its synthesis method and application
  • A kind of jatrorrhizine platinum (ii) complex and its synthesis method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

Embodiment 2

[0051] In a 50 mL round-bottomed flask, weigh 1.0 mol of derivative 2, 0.8 mol of potassium chloride, and 1.50 mol of lutidine amine, dissolve them in 5.0 ml of acetonitrile solution, and react at 90°C for 4 hours. The Jat2 ligand was obtained as a yellow solid powder with a yield of 81.0%.

[0052] In a 100.0 mL high pressure bottle, weigh 1.0 mol of the ligand Jat2 and an equal amount of dichloro-bis(dimethylsulfoxide) platinum(II), dissolve it in 5.0 mL of acetonitrile solution, and store at 60°C The coordination reaction was carried out at 4.0 h, washed with acetonitrile and then dried in vacuum at a temperature of 40° C. to obtain the yellow-brown target product Pt2. The yield was 90.8%.

Embodiment 3

[0054]The difference from Example 1 is that in a 100.0mL high-pressure bottle, 1.0mol of the ligand Jat1 and the amount of dichloro-bis(dimethylsulfoxide) platinum(II) are weighed, 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 then vacuum-dried 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 jatrorrhizine platinum (II) complex, a synthesis method thereof and an application of the complex in preparing antitumor drugs. The synthesis method of the jatrorrhizine platinum (II) complex comprises the following steps: (1) dissolving jatrorrhizine bromide derivatives, potassium chloride and lutidine amine in a solvent, and reacting at 90°C to obtain Yellow solid powder is Jat ligand; (2) Jat ligand prepared in step (1) and dichlorobis(dimethylsulfoxide) platinum (II) are dissolved in acetonitrile solution at 55-65 The coordination reaction is carried out at ℃; (3) the product is washed and dried to obtain the target product. For the first time, the present invention uses the jatrorrhizine derivative Jat as an active ligand to synthesize its platinum complex, which exhibits superior in vivo and in vitro anti-tumor activity and targeting, has potential medicinal value, and is expected to be used in various anti-tumor drugs preparation. The structural formula of the jatrorrhizine platinum (II) complex is as follows:

Description

technical field [0001] The invention relates to a platinum complex and a synthesis method thereof, in particular to a jatrorrhizine platinum (II) complex and a synthesis method thereof. The invention also relates to the application of the 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. Therefore, the development of new low-toxicity ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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