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Preparation method of meter platinum

A miplatin and cis technology, applied in the field of medicinal chemistry, can solve the problems of troublesome post-processing and long reaction time

Inactive Publication Date: 2010-12-01
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since myristic acid is soluble in chloroform and hardly soluble in water, the reaction is basically carried out in two phases, the reaction time is longer, and a variety of solvents are added, resulting in troublesome post-processing

Method used

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  • Preparation method of meter platinum
  • Preparation method of meter platinum

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1. Sodium myristate solubility test in water at different temperatures

[0031] A certain amount of sodium myristate was added to a certain volume of water, and its solubility was observed at different temperatures. The specific experimental content and results are shown in Table 1. As the temperature increases, the solubility of sodium myristate in water increases, and the solubility is better when the temperature is ≥50 °C.

[0032] Table 1. Solubility of sodium myristate in water at different temperatures

[0033]

Embodiment 2

[0034] Embodiment 2. The solubility test of sodium myristate in water and alkyl alcohol mixed solvent at the same temperature

[0035] In a certain amount of water and alcohol (volume ratio 1: 1) mixed solvent, at the same temperature, observe its dissolving ability to sodium myristate, concrete experiment content and result are shown in Table 2. The experimental results show that sodium myristate has certain solubility in the mixed solvent of water and alcohol at 30°C, and the solubility order of the mixed solvent is: water-isopropanol (1:1)>water-ethanol (1:1 )>water-methanol (1:1).

[0036] Table 2. Solubility of sodium myristate in mixed solvents of water and alkanol at the same temperature

[0037]

Embodiment 3

[0038] Embodiment 3. Solubility experiment of sodium myristate in water and ethanol mixed solvent in different proportions

[0039] At the same temperature, in mixed solvents of water and ethanol in different proportions, the dissolving ability of sodium myristate was observed. The specific experimental content and results are shown in Table 3. The experimental results show that no matter increasing or decreasing the ratio of ethanol in the mixed solvent at the same temperature, the solubility of sodium myristate will decrease, and the optimum ratio of sodium myristate dissolved in the mixed solvent of water and ethanol is 1:1.

[0040] Table 3. Solubility of sodium myristate in mixed solvents of water and ethanol in different proportions

[0041]

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Abstract

The invention relates to a preparation method of meter platinum, including that dinitric acid cis-((1R, 2R)-1, 2-diaminocyclohexane-dihydrate) platinum (II) and myristate react in solvent; wherein the solvent is composed of alkyl alcohol and water, the alkyl alcohol is methyl alcohol, ethyl alcohol, propyl alcohol or isopropyl alcohol, the myristate is sodium salt, kali salt or ammonium salt of myristic acid, reaction temperature is 20-80 DEG C, and the mass ratio of dinitric acid cis-((1R, 2R)-1, 2-diaminocyclohexane-dihydrate) platinum (II) and water is 1: 10-100. The volume ratio of water and alkyl alcohol is 1: 0.5-2 preferentially, and 1:1 more preferentially. The preparation method has simple steps, reaction medium can dissolve myristate, thus reaction can be effectively carried out and the method can be applied to industrialized production.

Description

technical field [0001] The invention relates to a preparation method of an antineoplastic drug miplatin, belonging to the technical field of medicinal chemistry. Background technique [0002] Miriplatin (miriplatin) is a fat-soluble platinum (II) antineoplastic drug, its code name is SM-11355, and its main indication is liver cancer. It was developed by Bristol-Myers-Squibb Company in the early stage, and later developed by Sumitomo Pharmaceutical Co., Ltd. It was developed and launched in Japan in 2009. The chemical structural formula of rice platinum is shown in formula (I), [0003] [0004] Formula (I) [0005] The preparation method reports about miplatin mainly relate to the following several patent methods. [0006] One is the method disclosed in European Patent Publication No. 0193936A1 (priority Japanese patent JP43869 / 85), and its chemical reaction formula is as follows. First remove the chloride ion in the starting material cis-[dichloro-(1R, 2R)-1,2-cycloh...

Claims

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Application Information

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IPC IPC(8): C07F15/00
Inventor 发明人公布姓名孙艳艳诸海滨徐刚
Owner SOUTHEAST UNIV
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