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Preparation method of miriplatin hydrate

A technology of meplatin and a synthesis method, which is applied in the field of preparation of platinum antitumor drug meplatin, can solve the problems of chloroform being harmful to human body and long reaction period, and achieve the effects of avoiding injury, short production period and high yield.

Inactive Publication Date: 2012-01-25
KUNMING UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has a long reaction cycle, and the chloroform used is harmful to the human body.

Method used

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  • Preparation method of miriplatin hydrate
  • Preparation method of miriplatin hydrate
  • Preparation method of miriplatin hydrate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Under normal temperature and pressure, according to the liquid-solid mass ratio of 1g: 3ml, K 2 PtCl 4 Soluble in water, according to K 2 PtCl 4 : KI is 1g: 1.6g ratio to weigh KI, then according to the liquid-solid mass ratio of 1g: 5ml, dissolve KI in water and add the KI solution to K under the condition of dark stirring 2 PtCl 4 solution, after 30 minutes of reaction, press K 2 PtCl 4 : (1R, 2R)-1,2 cyclohexanediamine is 1g:0.27g Weigh (1R,2R)-1,2 cyclohexanediamine, according to the liquid-solid mass ratio of 1g:3ml, the (1R, 2R)-1,2 cyclohexanediamine was diluted with water and added to the solution, reacted for 2 hours and filtered to obtain a yellow precipitate, washed the filter cake with water for 3 times and when the filtrate was neutral, washed the filter cake with absolute ethanol for 2 times, Then dry at 70°C to obtain PtC with purity ≥98% 6 h 14 N 2 I 2 .

[0026] See accompanying drawing technological process. Weigh 5.63 g of cycloplatinum, a...

Embodiment 2

[0030] Under normal temperature and pressure, according to the liquid-solid mass ratio of 1g:4ml, K 2 PtCl 4 Soluble in water, according to K 2 PtCl 4 : KI is 1g: 1.7g ratio to weigh KI, then according to the liquid-solid mass ratio of 1g: 6ml, dissolve KI in water and add the KI solution dropwise to K under the condition of dark stirring 2 PtCl 4 solution, after 30 minutes of reaction, press K 2 PtCl 4 : (1R,2R)-1,2 cyclohexanediamine is 1g:0.30g Weigh (1R,2R)-1,2 cyclohexanediamine, according to the liquid-solid mass ratio of 1g:4ml, the (1R, 2R)-1,2 cyclohexanediamine was diluted with water and added to the solution, reacted for 2 hours and filtered to obtain a yellow precipitate, first washed the filter cake with water for 4 times and the filtrate was neutral, then washed the filter cake with absolute ethanol for 3 times , and then dried at 70°C to obtain PtC with a purity ≥ 98% 6 h 14 N 2 I 2

[0031] See accompanying drawing technological process. Weigh 5.63g...

Embodiment 3

[0036] Under normal temperature and pressure, according to the liquid-solid mass ratio of 1g:5ml, K 2 PtCl 4 Soluble in water, according to K 2 PtCl 4 : KI is 1g: 1.8g ratio to weigh KI, and then according to the liquid-solid mass ratio of 1g: 8ml, dissolve KI in water and add the KI solution to K under the condition of avoiding light and stirring. 2 PtCl 4 solution, after reacting for 30min, press K 2 PtCl 4 : (1R,2R)-1,2 cyclohexanediamine is 1g:0.32g Weigh (1R,2R)-1,2 cyclohexanediamine, according to the liquid-solid mass ratio of 1g:5ml, the (1R, 2R)-1,2 cyclohexanediamine was diluted with water and added to the solution, reacted for 2 hours and filtered to obtain a yellow precipitate, first washed the filter cake with water for 5 times and the filtrate was neutral, then washed the filter cake with absolute ethanol for 4 times , and then dried at 70°C to obtain PtC with a purity ≥ 98% 6 h 14 N 2 I 2 .

[0037] See accompanying drawing process flow. Weigh 5.63g ...

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Abstract

The invention relates to a preparation method of an anticancer medicament, namely miriplatin hydrate, and belongs to the technical field of pharmaceutical chemistry. The preparation method comprises the steps of: hydrolyzing trans-diiodo-((1R ,2R)-1,2-hexamethylene diamine) platinum (II) (cycloplatin), serving as a reactant, by using silver sulfate, then reacting a hydrolyzed product with barium hydroxide to generate a trans-hydroxy-((1R, 2R)-1,2-hexamethylene diamine) platinum (II) solution, reacting the solution with tetradecanoic acid to obtain white precipitates, namely, solid miriplatin hydrate. The preparation method of the miriplatin hydrate in the invention has the advantages of short process flow, high yield, good product purity, no application of chloroform and other toxic solvents, simplicity and convenience for operation, and easiness for large-scale production.

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. Structural formula such as formula I. [0003] [0004] (I) [0005] Mibo is currently listed 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 reporte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00
Inventor 普绍平王庆琨胡劲丛艳伟孙加林
Owner KUNMING UNIV OF SCI & TECH
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