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New method for preparing picoplatin

A technology of picoplatin and picoline, which is applied in the field of preparation of anti-tumor drug picoplatin, can solve the problems of complicated production process requirements, increased manufacturing costs, complicated purification process, etc., and achieve the effect of convenient industrial production

Active Publication Date: 2010-07-14
NANJING CHENGONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] However, in the synthesis process, considering that the boiling point of NMP is 204°C, it is difficult to ensure recovery at 50°C-65°C even under reduced pressure, and increasing the temperature will inevitably lead to an increase in by-products, so the patent does not recover the solvent NMP but rather A large amount of dichloromethane, diethyl ether and other solvents are used to precipitate the product trichloro(2-picoline)potassium platinumate, and then the reaction of trichloro(2-picoline)potassium platinumate with ammonium hydroxide finally gives picoplatin
Though this method has avoided the generation of side reaction, trichloro (2-picoline) potassium platinum acid has certain dissolubility and can not precipitate completely in above-mentioned solvent, and a large amount of organic solvents that do not reclaim bring to production in addition Inconvenient, increased manufacturing costs, and complicated production process requirements
[0020] In summary, the shortcomings of the prior art for preparing picoplatin can be attributed to: since 2-picoline is a weakly basic substance, when it is combined with Potassium tetrachloroplatinate complex requires severe reaction conditions, which leads to a large loss of platinum in the preparation process, which inevitably brings complicated purification processes and expensive production costs

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0050] This example illustrates the preparation of picoplatin.

[0051] In the reaction flask, add K under dark conditions 2 PtCl 4 (103.8g, 0.25mol), 1500mL of deionized water, and 500mL of an aqueous solution in which KI (166g, 1mol) was dissolved was added, and the mixture was stirred at 25°C for 2 hours. 2-Methylpyridine (23.3 g, 0.25 mol) was slowly added dropwise, and the mixture was stirred at 25°C for 8 hours. Filter and dry under reduced pressure to obtain potassium triiodo(2-picoline)platinate(II) potassium (170.0 g, 0.24 mol) in the form of brown crystalline powder, with a yield of 96%, and store it in an airtight and dark place for future use;

[0052] Potassium triiodo (2-picoline) platinum (II) (170.0 g, 0.24 mol), 25% ammonia (16.3 g, 0.24 mol), and 2000 mL of deionized water were stirred at room temperature and protected from light. Mix evenly, stir at 25°C for 8 hours, filter, wash the filter cake with pure water, and dry under vacuum at 45°C to obtain cis-...

Embodiment 2

[0055] The preparation method of the picoplatin of this embodiment is the same as that of Example 1, but the reaction conditions are changed.

[0056] In the reaction flask, add K under dark conditions 2 PtCl 4 (103.8g, 0.25mol), 1500mL of deionized water, and 500mL of an aqueous solution in which KI (166g, 1mol) was dissolved was added, and the mixture was stirred at 30°C for 2 hours. 2-Methylpyridine (23.3 g, 0.25 mol) was slowly added dropwise, and the mixture was stirred at 30° C. for 8 hours. Filtrate and dry under reduced pressure to obtain potassium triiodo(2-picoline)platinate(II) potassium (163.0 g, 0.23 mol) in the form of brown crystalline powder, with a yield of 92%, and store it in an airtight and dark place for future use;

[0057] Potassium triiodo (2-picoline) platinum (II) (163.0 g, 0.23 mol), 25% ammonia (15.6 g, 0.23 mol), and 2000 mL of deionized water were stirred at room temperature and protected from light. Mix well, stir at 30°C for 8 hours, filter, ...

Embodiment 3

[0060] The preparation method of the picoplatin of this embodiment is the same as that of Example 1, but the reaction conditions are changed.

[0061] In the reaction flask, add K under dark conditions 2 PtCl 4 (103.8g, 0.25mol), 1500mL of deionized water, and 500mL of an aqueous solution in which KI (166g, 1mol) was dissolved was added, and the mixture was stirred at 15°C for 1 hour. 2-Methylpyridine (23.3 g, 0.25 mol) was slowly added dropwise, and the mixture was stirred at 15° C. for 8 hours. Filter and dry under reduced pressure to obtain potassium triiodo(2-picoline)platinate(II) potassium (172.0 g, 0.24 mol) in the form of brown crystalline powder, with a yield of 97%, and store it in a sealed and dark place for future use;

[0062] Potassium triiodo (2-picoline) platinum (II) (172.0 g, 0.24 mol), 25% ammonia (16.3 g, 0.24 mol), and 2000 mL of deionized water were stirred at room temperature and protected from light. Mix evenly, stir at 15°C for 8 hours, filter, wash...

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Abstract

The invention relates to a novel method for preparing picoplatin. The technical scheme adopts following steps of: firstly generating potassium tetraiodoplatinate by reacting potassium tetrachloro platinum with potassium iodide to improve the activity of reactants; generating triiodo (2-picoline) platinum (II) potassium by reacting the potassium tetraiodoplatinate with 2- picoline; generating Cis-2 iodine-ammonia and (2-picoline) platinum (II) by reacting triiodo (2-picoline) platinum (II) potassium with ammonia water; adding the Cis-2 iodine-ammonia and the (2-picoline) platinum (II) together to deionized water; stirring the deionized water for reaction at the room temperature; filtering silver iodide precipitate when the reaction is completed; and adding potassium chloride so as to gradually separate out crystallized products of the picoplatin. In the invention, the reaction is more complete, the utilization of the platinum and the yield are enhanced, the products do not have silver irons, and the problem that the silver irons are exceeded needs not to be worried.

Description

technical field [0001] The invention relates to a new preparation method of antitumor drug picoplatin, which belongs to the technical field of pharmaceutical engineering. Background technique [0002] Picoplatin is a new generation of platinum anticancer drugs developed after cisplatin, carboplatin and oxaliplatin. Picoplatin is also known as: picoplatin, JM473, AMD473, ZD0473, etc., the English name is Picoplatin, the chemical name is cis-dichloro-ammonia, (2-picoline) platinum (II), molecular weight: 376.16, CAS : 181630-15-9, its chemical structure is as follows: [0003] [0004] Picoplatin was first researched and developed by Canadian AmorMed company. It is designed to reduce drug resistance through steric hindrance effect. Compared with cisplatin, picoplatin 2-picoline replaces one ammonia of cisplatin, and the methyl group is located on Pt. - Above the N plane, the steric hindrance of the reaction between the drug and other substances is increased, and the speed...

Claims

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Application Information

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IPC IPC(8): C07F15/00
Inventor 郭昭
Owner NANJING CHENGONG PHARM CO LTD
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