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Method of preparing oxaliplatin

A technology for oxaliplatin and antitumor drugs, applied in chemical instruments and methods, compounds containing elements of Group 8/9/10/18 of the periodic table, organic chemistry, etc. hidden dangers and other problems, to achieve the effect of easy availability of raw materials and simple process

Active Publication Date: 2007-10-17
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] U.S. Patent US 5290961 A discusses in the background technology that the synthetic technique that contains silver nitrate, oxalic acid in the prior art exists problem is: silver ion exists in the product
There are different shortcoming in these methods; Such as adding silver nitrate hydrolysis reaction with cis-dichlorocyclohexanediamine platinum (II) or cis-diiodocyclohexanediamine platinum (II) as starting material, Then filter to remove the silver chloride precipitate, add potassium oxalate or sodium oxalate to the mother liquor, generate oxaliplatin aqueous solution after the reaction, and concentrate under reduced pressure to obtain the method of oxaliplatin product, which adopts multi-step chemical reaction, resulting in process complicated process
In the method of preparing oxaliplatin by reacting with silver oxalate in one step, since silver oxalate decomposes and turns black when exposed to light, it may cause an explosion when baked or impacted. It is a dangerous and unstable chemical raw material that cannot be easily obtained from the market. It is supplied on the Internet, so it must be used in production, which increases the steps of the production process on the other hand, and at the same time brings potential safety hazards in production

Method used

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  • Method of preparing oxaliplatin
  • Method of preparing oxaliplatin
  • Method of preparing oxaliplatin

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Put 10 g (0.0263 mol) of dichlorodiamine platinum; 8.49 g (0.0500 mol) of silver nitrate; 5.28 g (0.0394 mol) of sodium oxalate, and 0.85 L of deionized water into the reaction bottle, and put it under the protection of nitrogen atmosphere at 50 ° C. Light reaction for 6 hours, filter out insoluble matter, wash the filter cake 3 times with deionized water, concentrate the filtrate with a rotary evaporator until a large amount of crystals are precipitated, filter, wash the filter cake with purified water, absolute ethanol, and absolute ether successively, and then After drying in a vacuum oven at 60°C overnight, 8.98 g of finished oxaliplatin was obtained, with a yield of 86.0% and a purity of 98.92% by HPLC.

Embodiment 2

[0024] With diiododiammine platinum (II) 10g (0.0178mol); Silver nitrate 5.75g (0.0339mol); Potassium oxalate 7.26g (0.0437mol), deionized water 0.95L drops in the reaction bottle, under the protection of nitrogen atmosphere in React in the dark at 60°C for 4 hours, filter out the insoluble matter, wash the filter cake with purified water 3 times, concentrate the filtrate with a rotary evaporator until a large amount of crystals are precipitated, filter, and wash the filter cake with purified water, absolute ethanol, and absolute ether in sequence , and then dried overnight at 50° C. in a vacuum oven to obtain 6.29 g of finished oxaliplatin, with a yield of 88.9%. The purity by HPLC is 99.78%.

Embodiment 3

[0026] 10g (0.0178mol) of diiododiammine platinum (II); 6.04g (0.0356mol) of silver nitrate; 3.63g (0.0293mol) of ammonium oxalate, and 0.8L of deionized water were dropped into the reaction flask, and the React in the dark at 40°C for 8 hours, filter out the insoluble matter, wash the filter cake with purified water, concentrate the filtrate with a rotary evaporator until a large number of crystals are precipitated, filter, and wash the filter cake with purified water, absolute ethanol, and absolute ether in sequence, and then Dry in a vacuum oven at 60° C. overnight to obtain 5.80 g of off-white oxaliplatin crystals with a yield of 82.0% and a purity of 98.7% by HPLC.

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Abstract

The present invention relates to preparation method of anticancer drug oxaliplatin which comprise that material cis-dihalo(trans-(-)-1,2- diamino cyclohexane)platium(II), silver nitrate, univalent metal ion or ammonium oxalate and oxygen-free deionized water are together prepared for oxaliplatin in one step. The invention has a simple process, product is good in color, and material is easy to get which is fit for industrial production.

Description

technical field [0001] The invention relates to a preparation method of an anticancer drug oxaliplatin. Background technique [0002] Oxaliplatin was first disclosed in 1978, and the compound was claimed in US Patent No. 4169846 A, and the preparation method of the compound was given. The basic steps of the method are as follows: (1) reacting dichlorocyclohexanediammine platinum (II) with silver nitrate solution; (2) removing silver chloride precipitate; (3) adding dibasic acid such as oxalic acid to react. European patent EP 0625523 discloses a method for preparing oxaliplatin by reacting cis-dichlorocyclohexanediamine platinum (II) with silver oxalate as a raw material. [0003] US Patent No. 5,290,961 A discusses in the background art that the problem in the prior art synthesis process containing silver nitrate and oxalic acid is that silver ions exist in the product. In order to overcome the above problems, the patentee of this patent proposes a solution to remove exce...

Claims

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Application Information

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IPC IPC(8): C07F15/00
Inventor 孙飘扬陈永江陈建
Owner JIANGSU HENGRUI MEDICINE CO LTD
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