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Platinum complexes

A technology for platinum complexes and pharmaceutical preparations, applied in the field of platinum complexes and their preparation, can solve the problems of large side effects, low water solubility, short remission period and the like

Inactive Publication Date: 2009-07-01
NANJING SANHOME PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Platinum complexes have broad-spectrum anticancer activity and have become the first choice of anticancer drugs at home and abroad. Although they have good curative effects in the treatment of certain cancers, they still have obvious shortcomings, and their side effects are relatively large. Renal toxicity of platinum, bone marrow toxicity of carboplatin, and low water solubility, the aqueous solution is not stable enough, and the remission period is short

Method used

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Embodiment 1

[0064] Embodiment 1: Synthesis of cis-diiodo (1R, 2R)-1,2-trans cyclohexanediamine platinum

[0065] Add 100ml of water to dissolve 4.2g of potassium chloroplatinite, add 16.6g of potassium iodide in 20ml of aqueous solution, and stir at room temperature for 10 minutes in the dark under nitrogen, then add 1.1g of (1R,2R)-1,2-trans-cyclohexanediamine 5ml of aqueous solution, stirred at room temperature for 45 minutes, filtered, washed with water, ethanol, ether, and dried in vacuum at 40°C. Weighed 5.3g, yield: 94.1%.

Embodiment 2

[0066] Embodiment 2: cis-diiodoethylenediamine platinum synthesis

[0067] Dissolve 2g of potassium chloroplatinite in 40ml of water, add 4g of potassium iodide in 5ml of aqueous solution, pass nitrogen to avoid light and react at room temperature for 10 minutes, add dropwise 0.4g of ethylenediamine in 5ml of aqueous solution, after the dropwise addition, continue stirring for 4 hours, filter, The filter cake was washed with water, ethanol and ether, and dried under vacuum at 40°C. Weighed 1.9g, yield: 78.0%.

Embodiment 3

[0068] Embodiment 3: cis-diiodine diammine platinum is synthesized

[0069] Dissolve 2.1g of potassium chloroplatinite in 50ml of water, add 8.3g of potassium iodide in 10ml of aqueous solution under dark conditions, stir for 10 minutes, add ammonia water (25%-28%) dropwise, keep the pH at about 8, and react for 5 hours After filtering, the filter cake was washed with water, ethanol and ether, and dried under vacuum at 40°C. Weighing: 2.25g, yield: 93.2%.

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Abstract

The invention relates to platinum complexes of the upper right formula and pharmaceutically acceptable salts or solvates, wherein R1 and R2 are respectively and independently selected from H or C1-C4 alkyls, or R1 and R2 are coupled as shown by the lower right formula. X is selected from a 3,4-dinicotinic acid radical or a cis form aconitic acid radical; and Y which has the same case with Z is selected from a cinnamic acid radical, a ketoprofen acid radical, a chlorogenic acid radical, a caffeic acid radical or a ferulic acid radical; or Y is different from Z, wherein Y can be 1-methyl-3-pyridine carboxylic acid, and Z can be a sulfate radical. The invention also relates to a preparation method for the platinum complexes and application of the platinum complexes to the preparation of anticancer drugs.

Description

technical field [0001] The invention relates to a platinum complex and a preparation method thereof, and also relates to an application for preparing anticancer drugs. Background technique [0002] Cancer, also known as malignant tumor and tumor. Cancer is a leading cause of death worldwide. Of a total of 58 million deaths worldwide in 2005, cancer accounted for 7.6 million (or 13%) of all deaths. In the past 20 years, the cancer mortality rate in China has increased by 29.42%, and every 4-5 deaths in China have 1 death from cancer. Cancer causes economic losses of more than 100 billion yuan to China every year. However, most of the existing anticancer drugs have teratogenic, carcinogenic and mutagenic effects, and are highly toxic. Therefore, it is urgent to study new effective and low-toxic anticancer drugs. In 1969, Luxembourg (Rosenberg.B.) reported the anticancer activity of cisplatin for the first time. After that, countless scientific workers conducted extensive ...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/555A61K31/282A61P35/00
Inventor 王勇张仓张文萍滕再进祝兴勇
Owner NANJING SANHOME PHARMACEUTICAL CO LTD
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