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Water-soluble dipropofol and preparation method thereof

A dipofofol and water-soluble technology, applied in the field of water-soluble dipofol and its preparation, can solve the problems of increasing production cost, reducing product yield, small steric hindrance and easy generation of other by-products, etc.

Inactive Publication Date: 2010-10-20
李世系 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation method disclosed in this patent is easy to generate other by-products due to the small steric hindrance in the phosphorylation reaction, which reduces the product yield and is difficult to purify
Adopt the method of protecting group, increase production cost, be unfavorable for industrialized production

Method used

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  • Water-soluble dipropofol and preparation method thereof
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  • Water-soluble dipropofol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Synthesis of propofol 2-chloromalonate

[0027]

[0028] method one:

[0029] N 2 Under protection, add 16.4g (0.1mol) 2,6-diisopropylphenol, 200ml ether, 4. / g (0.2mol) sodium hydride in four-necked flask (with condenser tube and thermometer), react in 10 Stir at ℃ until there are no bubbles, then add 3.0 mol 2-chloromalonyl chloride dropwise to the reaction solution, track until the reaction is complete, filter the suspension, wash with ether, concentrate the ether under reduced pressure, and vacuum distill the remaining oil to obtain 2 - Propofol chloromalonate. The obtained substance is detected by a mass spectrometer (mass spectrometry data can provide information about the molecular weight and structure of the substance, and can qualitatively and quantitatively determine the sample). The obtained mass spectrometry data are, 1 H-NMR (D 6 -DMSO): δ1.29 (d, 24H, 8CH 3 ); 3.12 (m, 4H, 4CH); 5.10 (s, H, CH); 6.92 (m, 2H, 2CH); 7.21 (d, 4H, 4CH). The mass spect...

Embodiment 2

[0033] Synthesis of Dipropofol 2-Phosphate Sodium Malonate

[0034]

[0035] Add 0.1mol sodium phosphate, 0.1mol 2-propofol 2-chloromalonate and 100ml distilled water in the bottle, and magnetically stir under ice bath cooling. When the temperature in the bottle naturally drops to 15°C, add dropwise dimethyl sulfoxide ( DMSO) 80ml, the reaction temperature rises, control not to exceed 20°C, after adding, stir the reaction until complete, add 110ml of 95% ethanol dropwise to the solution, let it stand overnight, wash the obtained solid with alcohol once, and dry it in vacuum for 48h (40°C ), to get the product. The obtained substance is detected by a mass spectrometer (mass spectrometry data can provide information about the molecular weight and structure of the substance, and can qualitatively and quantitatively determine the sample). The obtained mass spectrometry data are, 1 H-NMR (D 6 -DMSO): δ1.29 (d, 24H, 8CH 3 ); 3.12 (m, 4H, 4CH); 5.14 (s, H, CH); 6.92 (m, 2H, 2C...

Embodiment 3

[0037] Synthesis of Propofol 2-chlorosuccinate

[0038]

[0039] method one:

[0040] N 2 Under protection, add 16.4g (0.1mol) 2,6-diisopropylphenol, 200ml ether, 4.8g (0.2mol) sodium hydride to a four-necked flask (equipped with a condenser tube and a thermometer), and react at 10°C Stir until there are no bubbles, then add 3.0mol 2-chlorosuccinyl chloride dropwise to the reaction liquid, track until the reaction is complete, filter the suspension, wash with ether, concentrate the ether under reduced pressure, and vacuum distill the remaining oil to obtain 2-chlorosuccinyl chloride Propofol Malonate. The obtained substance is detected by a mass spectrometer (mass spectrometry data can provide information about the molecular weight and structure of the substance, and can qualitatively and quantitatively determine the sample). The obtained mass spectrometry data are, 1 H-NMR (D 6 -DMSO): δ1.29 (d, 24H, 8CH 3 ); 2.75(d,2H,CH 2); 3.12 (m, 4H, 4CH); 4.94 (t, H, CH); 6.92...

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Abstract

The invention discloses water-soluble dipropofol and a preparation method thereof. The water-soluble dipropofol has a certain general formula structure. The preparation method comprises the following steps of: reacting propofol, dihalogen acid and derivative thereof to generate diester under the alkali condition, and reacting the diester, phosphoric acid, thiophosphoric acid and derivatives thereof to obtain the water-soluble dipropofol. By introducing two-molecule propofol, the water-soluble dipropofol reduces the intake of the phosphorus, and has quick response; and the preparation method has the advantages of easily obtained raw materials, mild reaction conditions, convenient operation and easy industrialized production. The prepared injection has good water solubility and high stability, and enlarges the using crowds of the medicament. The water-soluble dipropofol can overcome the defects that the propofol emulsion is instable on thermodynamics and dynamics, easy to pollute and propagate microbes and inconvenient to store and use, can reduce or remove injection pain, reduces the intake of the phosphorus, and has quick response.

Description

technical field [0001] The invention relates to the field of chemical industry and pharmacy, in particular to a water-soluble dipopofol and a preparation method thereof. Background technique [0002] Propofol is a widely used injectable anesthetic for general intravenous anesthesia. It has the excellent characteristics of quick onset, short action time, complete recovery, and easy control of dosage. However, because it is a fat-soluble compound, it is difficult to dissolve in water. At present, it is mainly administered intravenously in the form of fat emulsion. This fat emulsion has certain side effects, such as injection pain, lipid metabolism disorder, hyperlipidemia and susceptibility to infection. A water-soluble phosphoryl carboxylate propofol and derivatives reported in Chinese patent CN101633671A. In the phosphorylation reaction of the preparation method disclosed in this patent, other by-products are easily generated due to the small steric hindrance, which reduce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/09C07F9/165A61P23/00
Inventor 李世系王崇育
Owner 李世系
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