Method for preparing oxaliplatin

A technology of oxaliplatin and potassium tetrachloroplatinite, which is applied in the field of preparation of oxaliplatin, can solve the problems of complex oxaliplatin production process, affecting the treatment effect of patients, and high impurity content, so as to reduce drug prices , reducing medical costs, high purity effect

Inactive Publication Date: 2015-03-25
SHANGHAI JINHE BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, the traditional production process of oxaliplatin is complicated, the yield is low, the cost is high, and the impurity content is high, which affects the treatment effect of patients.

Method used

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  • Method for preparing oxaliplatin

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preparation example Construction

[0020] The preparation method of oxaliplatin of the present invention comprises the following steps:

[0021] Step 1, Potassium tetrachloroplatinite reacts with potassium iodide, (1R, 2R)-cyclohexanediamine to prepare iodoplatinum; potassium tetrachloroplatinite: potassium iodide: (1R, 2R)-cyclohexanediamine=1 : 4.0-6.0: 1.0-1.15 (molar ratio), preferably potassium tetrachloroplatinite: potassium iodide: (1R, 2R)-cyclohexanediamine=1:4.5:1.06. The reaction temperature in step 1 is controlled at 20-30°C, preferably 25°C. In step 1, the reaction liquid is filtered, and the filter cake is washed with purified water, and the last filtrate is pH=6-8 (preferably pH=7).

[0022] Step 2, the nitrate intermediate of ammonia platinum in step 1 and cuprous nitrate reaction obtains aminoplatinum; Iodine ammonia platinum: cuprous nitrate=1: 1~1.05 (molar ratio), preferably iodine ammonia platinum: cuprous nitrate =1:1.02. The reaction temperature in step 2 is controlled at 20-30°C, pref...

Embodiment 1

[0027] Add 35 g of potassium tetrachloroplatinite and 70 mL of purified water into the reaction flask, and stir to dissolve. Weigh 63g of potassium iodide, add 75mL of water to dissolve. Slowly add potassium iodide aqueous solution to potassium tetrachloroplatinite filtrate, and stir at room temperature for 30 min in the dark. Weigh 10.25 g of (1R,2R)-cyclohexanediamine and dissolve it in 70 mL of purified water, and add the solution to the solution of potassium tetrachloroplatinite. Replace the reaction bottle with nitrogen for 5 minutes, stir at room temperature, a brownish-yellow solid is precipitated, and the reaction is not less than 20 hours, and the reaction temperature is 20°C. The reaction solution was filtered, and the filter cake was washed with purified water (3×30 mL). The last filtrate was pH=6-8, and pumped until no liquid dripped out. Wash the solid with 10 mL of absolute ethanol, and pump until there is no liquid drop. Wash the filter cake with 10 mL of anh...

Embodiment 2

[0031] Add 3.5 g of potassium tetrachloroplatinite and 10 mL of purified water into the reaction flask, and stir to dissolve. Weigh 6.3g of potassium iodide, add 10mL of water to dissolve. Slowly add potassium iodide aqueous solution to potassium tetrachloroplatinite filtrate, and stir at room temperature for 30 min in the dark. Weigh 1.1 g of (1R,2R)-cyclohexanediamine and dissolve it in 10 mL of purified water, and add the solution into the solution of potassium tetrachloroplatinite. Replace the reaction bottle with nitrogen for 5 minutes, stir at room temperature, and a brownish-yellow solid precipitates out. The reaction is not less than 15 hours, and the reaction temperature is 25°C. The reaction solution was filtered, and the filter cake was washed with purified water (3×5 mL), and the last filtrate had a pH of 6-8, and was pumped until no liquid dripped out. Wash the solid with 5 mL of absolute ethanol, and pump until there is no liquid drop. Wash the filter cake wit...

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Abstract

The invention discloses a method for preparing oxaliplatin. The method comprises the following steps: I, performing reaction on tertpotassium chloroplatinite, potassium iodide and (1R,2R)-cyclohexanediamine to prepare diiododiam mineplatinumg; II, performing reaction on diiododiam mineplatinum obtained in the step I, and cuprous nitrate so as to obtain a nitrate middle body of amine platinum; and III, performing reaction on the nitrate middle body of the step II and sodium oxalate, thereby preparing oxaliplatin. By adopting the method, the production cost can be reduced, the medical expense of patients is reduced, the side effect is alleviated, and the yield is relatively high.

Description

technical field [0001] The invention relates to a preparation method of antitumor drugs, in particular to a preparation method of oxaliplatin. Background technique [0002] According to medical statistical surveys, in recent years, China has become the country with the highest new incidence rate of cancer patients in the world. The "2013 China Cancer Registration Annual Report" released by the National Cancer Registration Center also shows that in the past 20 years, cancer in my country has become younger and the incidence rate is higher. The incidence of tumors is increasing at a rate of 3%-5% per year. [0003] Oxaliplatin is called L-trans diaminocyclohexane oxaliplatin, Oxaliplatin, which is the third-generation platinum anticancer drug developed after cisplatin and carboplatin. Oxaliplatin is a stable, water-soluble platinum-based alkylating agent. It is the first cyclohexanediaminoplatinum compound to be marketed and the first platinum-based alkylating agent to be show...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00
CPCC07F15/0013
Inventor 张伟中王权勇张爱平吴玉娟仝泽彬蔡志香唐桂根
Owner SHANGHAI JINHE BIO TECH
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