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Method for preparing platinum(II) metal complex eptaplatin

A technology of metal complexes and complexes, which is applied to the active ingredients of heavy metal compounds, pharmaceutical formulations, chemical instruments and methods, etc., can solve the problems of difficult large-scale production, high product cost, expensive silver salts, etc., and achieves complete reaction, The effect of stable product quality and improved yield

Inactive Publication Date: 2006-06-21
JIANGSU DURUI PHARMACEUTICAL CO LTD
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  • Abstract
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  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The preparation method of above-mentioned platinum (II) type metal complex eplatin, aftertreatment is comparatively loaded down with trivial details: method 1 needs to adopt methods such as preparation high-performance liquid chromatography or anion exchange resin column method to process reaction mixture, to separate product; method 2 needs Use auxiliary diatomaceous earth filtration to process the reaction mixture; method 3 also needs to use preparative high performance liquid chromatography, or anion exchange resin column method, or auxiliary methods such as diatomaceous earth filtration to process the reaction mixture
Therefore, it is difficult to produce on a large scale; in addition, the price of silver salt is more expensive, about ten times the price of mercury salt, and the cost of the product is higher

Method used

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  • Method for preparing platinum(II) metal complex eptaplatin
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  • Method for preparing platinum(II) metal complex eptaplatin

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Malonic acid (5.2 grams, 0.05 moles) was dissolved in 100 milliliters of water, and 30 milliliters of aqueous solutions of potassium hydroxide (5.6 grams, 0.1 moles) were added to adjust the pH of the solution to about 8, stirred at room temperature for 1 hour, and under nitrogen protection, Add Hg(NO 3 ) 2 1 / 2H 2 O (16.68 g, 0.05 mol) was dissolved in 100 ml of an aqueous solution, and the mixture was stirred at room temperature for 2 hours in the dark under the protection of nitrogen. Filter and dry under reduced pressure to obtain 13.6 g of mercuric malonate powder, with a yield of 89.9%, which is sealed and protected from light for future use.

[0047]cis-diiodo-[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II) (6.23 g, 10 mmol ) and mercuric malonate (3.03 g, 10 mmol) in 750 ml of aqueous solution were suspended and stirred for 20 hours at 55° C. in a dark room, and the resulting mercuric iodide precipitate was filtered out. Add 10 milliliter...

Embodiment 2

[0057] cis-diiodo-[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II) (6.23 g, 10 mmol ) and the mercurous malonate salt (3.03 grams, 10 mmoles) obtained in Example 1 were in 750 milliliters of aqueous solutions, suspended and stirred for 32 hours at room temperature in a dark room at 25° C., filtered out the precipitate of mercurous iodide generated, The filtrate was filtered with a microporous membrane (0.22 μm). The filtrate was concentrated under reduced pressure until a large amount of white crystals were precipitated, filtered, and dried to obtain 3.56 g of eplatin, with a yield of 75.5%. The crude product was determined by HPLC: 93.8%.

Embodiment 3

[0059] cis-diiodo-[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]platinum(II) (6.23 g, 10 mmol ) and the mercurous malonate salt (3.03 grams, 10 mmoles) obtained in Example 1 were in 750 milliliters of aqueous solutions, suspended and stirred for 12 hours at 80° C. in a dark room, filtered out the precipitate of mercurous iodide generated, and the filtrate Then filter with a microporous membrane filter (0.22 μm). The filtrate was concentrated under reduced pressure until a large amount of white crystals precipitated, filtered, and dried to obtain 3.92 g of Epplatin, with a yield of 83.2%. The crude product was determined by HPLC: 96.7%.

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Abstract

The invention relates to the field of medicinal chemistry, in particular to a method for preparing anticancer drug platinum (II) metal complex eplatin. The present invention is characterized in that a platinum (II) type metal complex eplatin is obtained by reacting a dihalogenated diamine platinum complex with mercury malonate. Compared with the prior art, the present invention has the advantages of low cost, simple product separation, suitable for large-scale industrial production and the like.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation method of platinum (II) metal complex eplatin. Background technique [0002] Since the discovery of cisplatin's anticancer activity in 1967, the application and research of platinum(II) metal complex anticancer drugs have developed rapidly. In the past nearly 40 years, scholars from various countries have synthesized thousands of new platinum series compounds and entered into screening, more than 30 compounds have entered clinical research, 6 compounds have been approved to enter the market, and many more compounds Production approval will be obtained. At present, platinum (II) metal complexes are the most widely used anti-tumor drugs in the world today. Among the platinum (II) metal complexes that have been approved for clinical use, cisplatin (Cisplatin), carboplatin (Carboplatin), and Oxaliplatin and Nedaplatin have become indispensable drugs in cancer chemot...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D317/14C07F15/00A61P35/00A61K31/282A61K31/335
Inventor 陈庆宏施欣忠
Owner JIANGSU DURUI PHARMACEUTICAL CO LTD
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