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Water-soluble S, S-heptaplatin derivative

A water-soluble and derivative technology, applied in the directions of drug combination, drug delivery, organic active ingredients, etc., can solve the problem of high nephrotoxicity, and achieve the effects of high water solubility, low overall toxicity, and good clinical application prospects.

Active Publication Date: 2011-06-01
KUNMING INST OF PRECIOUS METALS +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, heptaplatin has relatively high nephrotoxicity, which is a dose-limiting toxicity, and many patients cannot tolerate it.

Method used

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Embodiment Construction

[0019] (1) Preparation of 3-hydroxyl-1,1-silver cyclobutane dicarboxylate

[0020] Firstly, 3-hydroxy-1,1-cyclobutane dicarboxylic acid (mp 151-152° C.) was prepared according to the method reported in the literature [Inorganica Chimica Acta, 2004, 357, 4452-4466]. Take 10g of 3-hydroxy-1,1-cyclobutanedicarboxylic acid, dissolve it in 100ml of water, adjust the pH to 5-6 with 1mol / L NaOH, add 100ml containing 130mmol AgNO 3 (5% excess) aqueous solution, 3-hydroxyl-1,1-cyclobutane dicarboxylate silver precipitate was obtained, collected by filtration, washed with water and ethanol, and then vacuum-dried at 60-70°C for 4 hours to obtain 21.7g of 3-hydroxyl- Silver 1,1-cyclobutanedicarboxylate, yield 94.2%.

[0021] (2) Preparation of diiodine intermediate

[0022] Weigh 5g K 2 PtCl 4 (12mmol) was dissolved in 50ml of water, and the insolubles were removed by filtration. At 30°C, 50ml of an aqueous solution containing KI 12g (72mmol) was slowly added, and after reaction in th...

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Abstract

The invention relates to a new water-soluble S, S-heptaplatin derivative-cis-[(4S, 5S)-4, 5-bi (aminomethyl)-2-isopropyl-1, 3-dioxolane 3-hydroxy-1, 1-cyclobutanedicarboxylate platinum (II)]. The derivative is prepared by the following steps of: (1) preparing a required amine ligand by using L-diethyl tartrate as an initial raw material through condensation, ammonolysis and LiAlH4 reduction reaction; and (2) adding LI to K2[PtCl4] used as an initial raw material, transforming the raw material into K2PtI4, making the K2PtI4 react with the amine ligand (4S, 5S)-4, 5-bi (aminomethyl)-2-isopropyl-1, 3-dioxolane to prepare a corresponding diiodo intermediate, and making the diiodo intermediate react with 3-hydroxy-1, 1-cyclobutanedicarboxylate in equimolar amounts to obtain a target compound. The compound has the characteristics that the antitumaous effect of the compound is higher than that of carboplatin, heptaplatin and R, R-derivatives thereof, and the toxicity is lower than that of carboplatin, heptaplatin and R, R-derivatives thereof. The compound can be used for treating cancers clinically. Moreover, the compound also has the advantages of good water solubility and stability, and can be prepared into lyophiled powder or aqueous solution.

Description

technical field [0001] The present invention relates to a novel water-soluble S, S-type heptaplatin derivative-cis-[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3- Dioxolane 3-hydroxyl-1,1-cyclobutane dicarboxylate platinum (II)] (English name: cis-[(4S,5S)-4,5-bis(aminomethyl)-2- The invention relates to isopropyl-1, 3-dioxolane·(3-hydroxy-1, 1-cyclobutanedicarboxylato) platinum (II)] and its use as an anticancer drug, belonging to the field of chemical pharmacy. Background technique [0002] Cancer is a disease that seriously threatens human health and life, and is the second leading cause of death in the world after cardiovascular disease. In recent years, in my country alone, there are 2.2 million new cancer cases and 1.6 million cancer deaths each year. Chemotherapy is one of the three major means of clinically dealing with cancer at present, so countries all over the world invest a lot of manpower, material resources and financial resources in the research and developm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00A61K9/19A61K9/08
Inventor 刘伟平楼丽广谌喜珠谢成英叶青松全海天
Owner KUNMING INST OF PRECIOUS METALS
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