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New oxaliplatin derivate

A technology for oxaliplatin and derivatives, applied in the field of oxaliplatin derivatives and their use as anticancer drugs, can solve the problems of high toxicity of oxaliplatin, and achieve the effect of good clinical application prospect and high water solubility.

Inactive Publication Date: 2008-10-22
KUNMING INST OF PRECIOUS METALS +1
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Problems solved by technology

However, oxaliplatin is more toxic, and its intravenous administration is the half lethal dose LD for ICR mice. 50 It is 19.8mg / kg, and the common toxic and side effects are neurotoxicity and digestive toxicity, wherein neurotoxicity is dose-limiting toxicity, and some patients have severe chemotherapeutic symptoms such as dementia, memory loss, tremor [Pasetto L.M., Oxaliplatin-related neurotoxicity: How and why? , Critical Reviews in Oncology / Hematology, 2006, 59, 159-168]

Method used

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Embodiment Construction

[0017] (1) Preparation of 2,2-bis(hydroxymethyl)-1,3-silver malonate

[0018] Using commercially available diethyl 2,2-bis(hydroxymethyl)-1,3-malonate as raw material, obtain 2,2-bis(hydroxymethyl)-1,3-malonate after hydrolysis . Take 10g of 2,2-bis(hydroxymethyl)-1,3-malonic acid, dissolve it in 100ml of water, adjust the pH to 6-7 with 1mol / L NaOH, add 128mmol AgNO 3 (Excessive 5%) solution 100ml, produce white precipitate, filter and collect, after washing with water, ethanol, vacuum-dry at 60-70 ℃ for 4 hours, obtain 2,2-bis(hydroxymethyl)-1,3-malonic acid Silver 21g, yield 91%.

[0019] (2)cis-[Pt(II)A 2 I 2 ] Preparation of intermediate

[0020] Weigh 5g K 2 PtCl 4 (12mmol) was dissolved in 50ml of water, and the insolubles were removed by filtration. At 40°C, 50ml of an aqueous solution containing KI 12g (72mmol) was slowly added, and after reaction in the dark for 1 hour, an equimolar (12mmol) of 1R, 2R-ring Hexanediamine (A 2), a yellow precipitate was obtain...

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Abstract

The invention relates to a novel oxaliplatin derivative of (1R, 2R-cyclohexanediamine.2, 2-Bis (hydroxymethyl)-1, 3-malonato-platinum (II)) and ((1R, 2R-cyclohexanediamine).2, 2-Bis (hydroxymethyl)malonato-platinum (II)). The derivative is prepared with the steps that the cis-(PtA2I2) (A2 is equal to 1R, 2R-cyclohexanediamine) is adopted as the raw material and quantitatively reacts with the 2, 2-Bis (hydroxymethyl)-1, 3-malonate silver, and a crude product then is obtained through the mother liquor concentration and freeze-drying after the AgI is filtered and separated; a pure product is obtained by recrystallizing the crude product in a system that the ratio of water to ethanol is 1:1. The anti-caner activity of the complex of the derivative is obviously higher than the oxaliplatin and the toxic side effect is obviously less than the oxaliplatin, and can be prepared into freeze-dried powders or injections and used for treating the cancer clinically.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a novel oxaliplatin derivative and its application as an anticancer drug. Background technique [0002] Cancer is a major disease of human beings, which seriously threatens people's health and safety, and has become a difficult problem for human beings to overcome. Chemotherapy is currently one of the three major means of clinical treatment of cancer. Therefore, countries around the world invest a lot of manpower, material and financial resources in the research and development of anticancer drugs for chemotherapy every year. Many achievements have been made to improve the efficiency of cancer treatment. The progression time of the disease is prolonged, and the overall survival period and quality of life of the patients are significantly improved [Edited by Han Rui and Sun Yan, Chemoprevention and Drug Therapy of Cancer in the New Century, People's Military Medical Publishing ...

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 刘伟平楼丽广谌喜珠叶青松侯树谦余尧
Owner KUNMING INST OF PRECIOUS METALS
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