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Method for preparing oxaliplatin

A technology of oxaliplatin and cis, which is applied in the field of preparation of oxaliplatin, can solve the problems of high chiral enantiomer residues and unfavorable production of chemical raw materials, and achieve high purity, increased yield, and low silver residues Effect

Active Publication Date: 2010-11-24
CHONGQING TAIHAO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the preparation process of oxaliplatin, the residual chiral enantiomer is high, which is very unfavorable to the production of chemical raw materials

Method used

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  • Method for preparing oxaliplatin

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Experimental program
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Effect test

Embodiment 1

[0044] 20 g of cis-dichloro(L-trans-1,2-cyclohexanediamine) platinum was heated and stirred in purified water to dissolve, and the temperature was controlled at 60°C to 80°C. Slowly add 22 grams of silver nitrate under the condition of avoiding light and stirring, and continue to stir and react for 2 hours. After the reaction, the reaction solution was cooled to room temperature, filtered with suction, and the filtrate was collected. Add excess saturated sodium chloride solution to the filtrate, stir, filter, and collect the filtrate. Add ammonia water to the filtrate to adjust the pH=11, then add 14 grams of sodium oxalate, control the temperature at 65°C to 70°C, stir and react for 4 hours, concentrate the reaction solution under reduced pressure to 1 / 3 of the original volume, and cool it at 2 to 8°C Crystallize for 10 to 20 hours; when the crystallization is completed, the feed liquid is suction-filtered to obtain a filter cake, which is vacuum-dried at 75° C. to 80° C. fo...

Embodiment 2

[0046] 20 g of cis-dichloro(L-trans-1,2-cyclohexanediamine) platinum was heated and stirred in purified water to dissolve, and the temperature was controlled at 65°C to 70°C. Slowly add 20 grams of silver nitrate under the condition of avoiding light and stirring, and continue to stir and react for 2 hours. After the reaction, the reaction solution was cooled to room temperature, filtered with suction, and the filtrate was collected. Add excess saturated sodium chloride solution to the filtrate, stir, filter, and collect the filtrate. Add ammonia water to the filtrate to adjust pH=10, then add 10 grams of sodium oxalate, control the temperature at 60°C-80°C, stir and react for 4 hours, concentrate the reaction solution under reduced pressure to 1 / 3 of the original volume, and cool it at 2-8°C Crystallize for 10-20 hours; when the crystallization is completed, the feed liquid is suction-filtered to obtain a filter cake, which is vacuum-dried at 75° C. to 80° C. for 5 hours to ...

Embodiment 3

[0048] 20 g of cis-dichloro(L-trans-1,2-cyclohexanediamine) platinum was heated and stirred in purified water to dissolve, and the temperature was controlled at 60°C to 80°C. Slowly add 18 grams of silver nitrate under the condition of avoiding light and stirring, and continue to stir and react for 2 hours. After the reaction, the reaction solution was cooled to room temperature, filtered with suction, and the filtrate was collected. Add excess saturated sodium chloride solution to the filtrate, stir, filter, and collect the filtrate. Add ammonia water to the filtrate to adjust the pH=9, then add 7 grams of sodium oxalate, control the temperature at 60°C-80°C, stir and react for 4 hours, concentrate the reaction solution under reduced pressure to 1 / 3 of the original volume, and cool it at 2-8°C Crystallize for 10-20 hours; when the crystallization is completed, the feed liquid is suction-filtered to obtain a filter cake, which is vacuum-dried at 75° C. to 80° C. for 5 hours t...

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Abstract

The invention relates to the field of pharmaceutical engineering and discloses a method for preparing oxaliplatin. The method comprises the following steps of: reacting aqueous solution of cis-((1R,2R)-(-)-1,2-diaminocyclohexaneplatinum)dichloride with silver nitrate under the shading and heating conditions; filtering and adding the excessive saturated solution of sodium chloride into the filtrate for reaction and filtering; adding ammonia water and sodium oxalate into the filtrate and reacting under the heating condition; and concentrating and crystallizing to obtain a crystal, and purifyingthe crystal by using activated carbon, wherein the molar ratio of the cis-((1R,2R)-(-)-1,2-diaminocyclohexaneplatinum)dichloride to the silver nitrate is 1:2-2.5, and the molar ratio of the cis-((1R,2R)-(-)-1,2-diaminocyclohexaneplatinum)dichloride to the sodium oxalate is 1:1-2. The method for preparing the oxaliplatin of the invention has a high yield, and the oxaliplatin product prepared by the method has the advantages of no chiral enantiomer, a little residual silver, high purity and suitability for industrial production when used as a chemical raw material medicament.

Description

technical field [0001] The invention relates to the field of pharmaceutical engineering, in particular to a method for preparing oxaliplatin. Background technique [0002] Oxaliplatin, also known as oxaliplatin, its English name is Oxaliplatin, its chemical name is (1R-trans)-(1,-2cyclohexanediamine-N,N')[oxalic acid (2-)-O, O'] combined with platinum, the molecular formula is C 8 h 14 N 2 o 4 Pt, its structure for: [0003] [0004] Oxaliplatin is the third generation of platinum-based anticancer drugs after cisplatin and carboplatin. It was first developed by Debiopharm in Switzerland, produced by Sanofi in France and first launched in France in October 1996, and then successively in Europe and other countries in South America. Oxaliplatin exhibits broad-spectrum cytotoxicity in vitro and antitumor activity in vivo in a variety of tumor model systems, especially in colon and rectal malignant tumor models. As the third generation of platinum drugs, oxaliplatin n...

Claims

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Application Information

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IPC IPC(8): C07F15/00
Inventor 李靖陈波杨显梅应振培
Owner CHONGQING TAIHAO PHARM CO LTD
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