Novel water soluble Pt (II) anti-cancer ligand and its preparing method

A technology of complexes and substituents, which is applied in the field of platinum anticancer complexes and their preparation, can solve the problems of high toxicity and side effects, and the overall curative effect is not as good as that of carboplatin, and achieve the effects of simple operation, high yield and pure product

Inactive Publication Date: 2006-08-23
KUNMING GUIYAN PHARMA
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Problems solved by technology

Although some new platinum-based anticancer drugs have been introduced in recent years, such as Nadaplatin, Oxaliplatin, Eptaplatin, and Loplatin, their water solubility is low. Compared with carboplatin, its comprehensive curative effect is not as good as carboplatin and its toxic and side effects are greater than carboplatin [You Qidong, Gou Shaohua, Research Progress of Anti-

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  • Novel water soluble Pt (II) anti-cancer ligand and its preparing method
  • Novel water soluble Pt (II) anti-cancer ligand and its preparing method
  • Novel water soluble Pt (II) anti-cancer ligand and its preparing method

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[0018] (1) Preparation of 3-hydroxyl-1,1-silver cyclobutane dicarboxylate

[0019] Firstly, 3-hydroxy-1,1-cyclobutanedicarboxylic acid (mp 151°C-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 6-7 with 1mol / L NaOH, add 130mmol, 100ml of AgNO 3 (excessive 5%), 3-hydroxy-1,1-cyclobutane dicarboxylate silver precipitate was obtained, collected by filtration, washed with water and ethanol, and dried under vacuum at 60-70°C for 4 hours to obtain 21.7g 3-hydroxy- Silver 1,1-cyclobutanedicarboxylate, yield 94.2%.

[0020] (2)cis-[Pt(II)A 2 I 2 ] Preparation of intermediate

[0021] [J.Med.Chem., 1994,37,1471-1485] synthetic carrier group A according to the process route reported in the literature 2 [A 2 =2-methyl-(4R,5R)-4,5-bis(aminomethyl)-1,3-dioxolane; 2-ethyl-(4R,5R)-4,5-bis( aminomethyl)-1,3-dioxol...

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Abstract

The present invention relates to a new kind of water soluble anticancer Pt (II) compound, cis-[2-substitutent- (4Rú¼5R)-4ú¼5-bis(aminoethyl)-lú¼3-dioxycyclopentaneíñ3-hydroxy-1ú¼1-cyclobutane dicarboxylic radical- Pt (II)], with the substitutent being methyl, ethyl or isopropyl radical. One of the preparation process includes the reaction of material cis-[PtA2I2], with A2 being 2-substitutent- (4Rú¼5R)-4ú¼5-bis(aminoethyl)-lú¼3-dioxycyclopentane, and 3-hydroxy-1ú¼1- cyclobutane dicarboxyl-Ag, filtering to separate AgI, concentrating the mother liquid and freeze drying to obtain the coarse product. The other preparation process includes the first reaction of cis-[PtA2I2] and Ag2SO4, filtering to separate AgI, the reaction of the mother liquid and 3-hydroxyl-1ú¼1-cyclobutane dicarboxylic Ba, filtering to separate BaSO4, concentrating mother liquid, and freeze drying to obtain the coarse product. The coarse product is re-crystallized in water/alcohol system to obtain refined product. The compound of the present invention has anticancer activity and less toxic side effect, and may be clinical use for treating cancers.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to a class of water-soluble platinum (II) anticancer complexes and a preparation method thereof. Background technique [0002] Carboplatin is the second-generation platinum anticancer drug after cisplatin, and its chemical name is cis-1,1-cyclobutane dicarboxylate · diammine platinum (II). The structure of carboplatin retains the anticancer active part (NH 3 ) 2 Pt 2+ , and introduce hydrophilic 1,1-cyclobutane dicarboxylate as leaving group, the solubility is greatly improved, the water solubility reaches 17mg / ml, which is 17 times higher than the solubility of cisplatin (1mg / ml), so card The toxicity of platinum, especially nephrotoxicity and gastrointestinal side effects, is significantly lower than that of cisplatin, making carboplatin one of the most effective anticancer drugs recognized in the world. In the pharmacopoeias of most countries in the world, it is widely used ...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/282A61K9/08A61K9/14A61P35/00
Inventor 楼丽广刘伟平谌喜珠侯树谦李永年
Owner KUNMING GUIYAN PHARMA
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