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Process for producing platinum

A technology of miplatin and cis, which is applied in the field of medicinal chemistry, can solve the problems of production personnel and environmental impact, and achieve the effects of low production cost, convenient product separation, and reduced treatment costs

Inactive Publication Date: 2009-04-08
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method uses solvents such as chloroform and lower alkanols, which will inevitably have a certain impact on production personnel and the environment

Method used

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  • Process for producing platinum
  • Process for producing platinum
  • Process for producing platinum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Preparation of Miplatin:

[0021] Add 5.2g of cis-dinitrate [(1R,2R)-1,2-cyclohexanediamine] platinum(II) (0.012mol) and 100ml of water into a 250ml reaction flask, stir, heat to 50°C, and keep warm Add 6.3 g (0.025 mol) of sodium myristate until the solid is dissolved and clear, and react at 50°C for 2 hours, cool to room temperature, filter the precipitated solid, wash the filter cake with water, and dry under vacuum at 40°C to obtain the target product (monohydrate) 8.3 g, yield: 88.4%.

[0022] Chemical purity: 99.28%. (HPLC conditions: use octadecylsilane bonded silica gel as filler; mobile phase is phosphate buffer [1.36g potassium dihydrogen phosphate is added in 10ml tetrabutylammonium hydroxide solution (32%), add water and dilute to 1000ml, use Adjust the pH value to 6.0 with phosphoric acid]-methanol (70:30); the flow rate is 1.0ml / min; the detection wavelength is 216nm.)

[0023] Optical purity: 100%. (HPLC condition: adopt chiral chromatographic column ...

Embodiment 2

[0029] The preparation of cis-dinitrate [(1R, 2R)-1,2-cyclohexanediamine] platinum (II):

[0030] Refer to the methods disclosed in documents such as patent EP567438 or EP617043:

[0031] Add cis[((1R,2R)-1,2-cyclohexanediamine-dichloro]platinum 25g (0.066mol) and water 500ml into a 1L reaction flask, stir, add silver nitrate 22.3g (0.13mol), Stir the reaction for 24 hours, remove the silver chloride solid by filtration, remove most of the water by distillation under reduced pressure at 50°C (ethanol with water can be used), cool to room temperature, filter the precipitated solid, wash the filter cake with water, and dry under vacuum at 40°C to obtain the white target product 25.9 g, yield: 90.6%.

Embodiment 3

[0033] Preparation of Miplatin:

[0034] Add 2.5g of cis-dinitrate [(1R,2R)-1,2-cyclohexanediamine] platinum(II) (5.8mmol) and 125ml of water into a 500ml reaction bottle, stir until the solid is dissolved and clarified, add meat Sodium myristate 2.9g (11.6mmol), react at room temperature for 7 hours, filter the precipitated solid, wash the filter cake with water, and vacuum dry at 40°C to obtain 3.5g of the target compound (monohydrate), yield: 77.2%. Chemical purity: 99.27%, optical purity: 100%.

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Abstract

The invention relates to a preparation method of Miboplatin. In the preparation method, Cis-dinitrate ((1R, 2R)-1, 2-cyclohexanediamine)platinum (II) is taken as starting materials and added with purified water to react with myristate with a general chemical formula of CH3(CH2)12COOM (M refers to Na, K and NH4) for 0.5h to 8h, and then cooled to the room temperature, filtrated and dried to obtain the Miboplation, wherein, the reaction temperature is 10 DEG C to 80 DEG C; the purified water added is 5 times to 50 times the weight of the Cis-dinitrate ((1R, 2R)-1, 2-cyclohexanediamine)platinum (II); and the mol ratio of the Cis-dinitrate ((1R, 2R)-1, 2-cyclohexanediamine)platinum (II) and the myristate is 1:2.0 to 3.0. The preparation method uses no toxic solvent such as chloroform and the like and is simple in operation, high in quality of products prepared and yield and low in cost. Simultaneously, the preparation method is applicable to commercial production.

Description

technical field [0001] The invention relates to a preparation method of miplatin, which belongs to the technical field of medicinal chemistry. Background technique [0002] Miriplatin English common name is Miriplatin (code name: SM-11355), chemical name: cis[((1R,2R)-1,2-cyclohexanediamine-N,N')bis(tetradecanoyloxy base)] platinum (II) and its hydrate. Miplatin is a fat-soluble platinum anticancer drug developed by Sumitomo Pharmaceutical Co., Ltd., Japan. It is considered to have therapeutic effects on solid tumors such as liver cancer, malignant lymphoma, non-small cell lung cancer, small cell lung cancer, and bladder cancer. Its structural formula Such as formula (I): [0003] [0004] Patent WO94 / 14470 discloses a series of preparation methods of fat-soluble platinum complexes, wherein the synthetic method of rice platinum is to react (1R, 2R)-1,2-cyclohexanediamine with potassium iodoplatinite to prepare cisplatin [((1R,2R)-1,2-Cyclohexanediamine-diiodo]platinum,...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
Inventor 宗在伟赵俊王孝雯魏佳陈卫东
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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