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New method for synthesizing anti-tumor drug miboplatin

A technology of miplatin and substances, which is applied in the field of preparation of platinum anti-tumor drug miplatin, which can solve the problems of greater harm to the human body and the environment, excessive silver ions, etc., and achieve the effects of short production cycle, avoiding damage, and high yield

Active Publication Date: 2012-11-07
KUNMING GUIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In the production process of platinum antineoplastic drugs, silver ions are one of the main reasons that affect the quality of drugs. The above-mentioned methods use silver complexes in the production process, which may easily cause excessive silver ions, and also used in foreign patents. Chloroform is more harmful to human body and environment

Method used

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  • New method for synthesizing anti-tumor drug miboplatin

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Experimental program
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Embodiment 1

[0024] Weigh 8.3gK 2 PtCl 4 , dissolved in water and filtered off the insoluble matter, weighed 7gNaNO 2 , dissolved in water and added to K 2 PtCl 4 In solution, react at 70°C for 6h to obtain light yellow K 2 Pt(NO 2 ) 4 solution. Weigh 2.8g (1R,2R)-1,2-cyclohexanediamine, dissolve it in water and add it dropwise to K 2 Pt(NO 2 ) 4 In the solution, after reacting at room temperature for 5 h, the obtained solid was filtered and dried to obtain 7.3 g of cis-dinitroso-(1R,2R)-1,2-cyclohexanediamine platinum(II) solid. Weigh 5g of hydrazine sulfate and dissolve it in 100ml of hot water, add 7.3g of cis-dinitroso-(1R,2R)-1,2-cyclohexanediamine platinum (II) solid, heat in a water bath for 3 hours and then cool , a small amount of solid was filtered to obtain a pale yellow hydrolyzed solution. Take by weighing 10g sodium tetradecanoic acid, dissolve it with 100ml n-butanol and add it dropwise in the hydrolysis solution, react at room temperature for 7h, filter the w...

Embodiment 2

[0026] Weigh 8.3gK 2 PtCl 4 , dissolved in water and filtered off the insoluble matter, weighed 7.5gNaNO 2 , dissolved in water and added to K 2 PtCl 4 In solution, react at 65°C for 6h to obtain light yellow K 2 Pt(NO 2 ) 4 solution. Weigh 2.3g (1R,2R)-1,2-cyclohexanediamine, dissolve it in water and add it dropwise to K 2 Pt(NO 2 ) 4 In the solution, after reacting at room temperature for 5 h, the obtained solid was filtered and dried to obtain 7.1 g of cis-dinitroso-(1R,2R)-1,2-cyclohexanediamine platinum(II) solid. Weigh 6g of hydrazine sulfate and dissolve it in 100ml of hot water, add 7.1g of cis-dinitroso-(1R,2R)-1,2-cyclohexanediamine platinum (II) solid, heat in a water bath for 4h and then cool , a small amount of solid was filtered to obtain a pale yellow hydrolyzed solution. Weigh 12g of sodium tetradecanoic acid, dissolve it with 120ml of n-butanol and add it dropwise to the hydrolysis solution. After reacting at room temperature for 7 hours, filter...

Embodiment 3

[0028] Weigh 8.3gK 2 PtCl 4 , dissolved in water and filtered off the insoluble matter, weighed 7.5gNaNO 2 , dissolved in water and added to K 2 PtCl 4 In solution, react at 60°C for 7h to obtain light yellow K 2 Pt(NO 2 ) 4 solution. Weigh 2.3g (1R,2R)-1,2-cyclohexanediamine, dissolve it in water and add it dropwise to K 2 Pt(NO 2 ) 4 In the solution, after reacting at room temperature for 7 hours, the obtained solid was filtered and dried to obtain 7.5 g of cis-dinitroso-(1R,2R)-1,2-cyclohexanediamine platinum(II) solid. Weigh 6.5g of hydrazine sulfate and dissolve it in 100ml of hot water, add 7.5g of cis-dinitroso-(1R,2R)-1,2-cyclohexanediamine platinum (II) solid, and heat in a water bath for 3.5h After cooling, a small amount of solid was filtered to obtain a pale yellow hydrolyzed solution. Weigh 12g of sodium tetradecanoic acid, dissolve it with 150ml of n-butanol and add it dropwise to the hydrolysis solution. After reacting at room temperature for 8 ho...

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Abstract

The invention relates to a preparation method of anti-tumor drug miboplatin, which comprises the process flow: based on K4PtC14 as a starting material, reacting K4PtC14 with sodium nitrite to generate a K4Pt(NO2)4 solution; reacting with (1R, 2R)-1, 2-cyclohexanediamine to generate cis-dinitroso-(1R, 2R)-1, 2-cyclohexanediamine platinum (II); and reducing NO2<-> using hydrazine sulfate, and reacting the obtained solution with n-butanol solution of sodium n-tetradecyl carbonate to generate miboplatin. In the method, silver ions are not introduced and toxic solvents such as chloroform are not used.

Description

technical field [0001] The invention relates to the preparation of platinum-based antitumor drug miplatin, belonging to the technical field of medicinal chemistry. Background technique [0002] Milplatin (SM-11355) is a new type of lipophilic platinum antineoplastic drug, the chemical name is cis[((1R,2R)-1,2-cyclohexanediamine-N,N′)bis(n-tetradecyl Carbonic acid)] platinum (II) and its hydrate. It is a fat-soluble platinum-based antineoplastic drug developed by Sumitomo Pharmaceutical Co., Ltd. of Japan, and is mainly used for the treatment of liver cancer. The structural formula is as follows: [0003] [0004] Mibo is currently approved for marketing in Japan. Miplatin is characterized by good fat solubility and low toxicity and side effects. The effective rate of miplatin-iodol emulsion for advanced liver cancer is 56%. The main toxicity is neutropenia and total bilirubin elevation. Well tolerated. For its preparation: the synthesis method route of miplatin repor...

Claims

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Application Information

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IPC IPC(8): C07F15/00
Inventor 王庆琨普绍平李永年何键栾春芳彭娟黄天俊张琪
Owner KUNMING GUIYAN PHARMA
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