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Preparation of novel organic platinum complex and uses thereof

A platinum complex and complex technology, which can be used in medical preparations containing active ingredients, organic chemistry, organic active ingredients, etc., can solve the problem of no compound nephrotoxicity or neurotoxicity.

Inactive Publication Date: 2009-05-13
BAIBO FANGZHOU BEIJING TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical trials have also shown that the compound is better tolerated than older platinum-based drugs, and no evidence of nephrotoxicity or neurotoxicity has been found so far

Method used

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  • Preparation of novel organic platinum complex and uses thereof
  • Preparation of novel organic platinum complex and uses thereof
  • Preparation of novel organic platinum complex and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0051] Synthesis of trichloro-2-picoline platinum (II) (4):

[0052] Add 0.83g (2mmoles) K to a 100ml one-necked flask 2 PtCl 4 and dry DMF (dimethylformamide), 0.21 ml (2.1 mmoles) of 2-methylpyridine was added dropwise under magnetic stirring at room temperature, and then the temperature was raised to 75° C. for 3 hours to react. After removal of DMF under reduced pressure, 100 ml of dichloromethane was added, and a solid was obtained by filtration. The solid was added to 100ml of acetone and dissolved under reflux, cooled to room temperature and then filtered. After evaporating the acetone to dryness, trichloro-2-picoline platinum(II)(4) was obtained, weighing 0.74g. Yield 85%.

[0053] Synthesis of cis-ammonia, 2-picoline dichloroplatinum(II) (6):

[0054] 0.54g (1.24mmoles) of compound (4) and 1ml of 2.5NKCl aqueous solution were added to a 10ml reaction flask, 0.83g of ammonium acetate trihydrate was added to 2.5ml of 2.5N ammonia water, and then added to the reactio...

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Abstract

The invention relates to preparation and application of a novel organo-antimony complex (1). The complex (1) has the characteristics of high anticancer activity, large water solubility, small toxic side effect and the like. A drug effect composition containing the complex (1) is used for treating various solid cancers, such as lung cancer, gastric carcinoma, liver cancer, breast carcinoma, cancer of colon, ovarian cancer, cervical carcinoma, leukemia, lymphoma, nasopharyngeal darcinoma and the like.

Description

technical field [0001] The invention relates to the preparation and application of a novel organic platinum complex, which has anticancer effect. Background technique [0002] Among the existing anticancer drugs, platinum drugs such as cisplatin (Cisplatin) and carboplatin (Carboplatin) occupy an important position. The second-generation and third-generation organic platinum drugs developed later, such as Oxaliplatin, Nedaplatin, Lobaplatin and Heptaplatin, are currently used as first- and second-line anticancer drugs. It has been widely used clinically. However, the activity of these complexes does not surpass that of cisplatin and carboplatin, and they still cannot effectively overcome the disadvantages of toxic side effects and cross-resistance. [0003] [0004] Cisplatin Carboplatin [0005] In order to overcome the above shortcomings, people have carried out a lot of research and development work, such as the new mixed amine dicarboxylic acid tetravalent platinum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61K31/282A61P35/00
Inventor 王松发姚辉
Owner BAIBO FANGZHOU BEIJING TECH
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