Substituted phenol for methylal phosphate anesthetic and sedative drugs and preparation method thereof

A technology of methylal phosphate disodium salt and acetal phosphate, which is applied in the field of phenol-substituted methylal phosphate anesthesia and sedative medicinal compounds and can solve the problems of difficult control of water content, strong hygroscopicity, and quality problems. Standard Difficulties and Other Issues

Active Publication Date: 2013-10-23
SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] In view of the above situation, the present invention will provide a phenol-substituted methylal phosphate anesthetic and sedative medicinal compound, especially a water-soluble precursor medicinal compound of a new form of propofol phosphate disodium salt, and the A preparation method of the compound, to satisfactorily solve the problem that the compound of formula (III) is difficult to control its moisture content and formulate its quality standard due to its strong hygroscopicity

Method used

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  • Substituted phenol for methylal phosphate anesthetic and sedative drugs and preparation method thereof
  • Substituted phenol for methylal phosphate anesthetic and sedative drugs and preparation method thereof
  • Substituted phenol for methylal phosphate anesthetic and sedative drugs and preparation method thereof

Examples

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Effect test

Embodiment 1

[0022] Add 13.0g of propofol phosphate disodium salt (commercially purchased or prepared according to the current literature method) into a 50ml single-mouth bottle, add 40ml of water and stir to dissolve at 50°C, add an appropriate amount of activated carbon to decolorize for 15 minutes after complete dissolution, filter, and dissolve 400ml of acetone Add it to the filtrate under stirring, stir to room temperature and place it under refrigeration until the crystallization is complete. Filtrate, wash with a small amount of acetone, and dry to obtain 16.1 g of white crystals of propofol phosphate disodium salt hydrate. After drying at 105°C to constant weight, the water content was 35%, and the yield was 80.5%. The infrared absorption spectrum was measured by the potassium bromide tablet method (instrument: American NICOLET MX-1 FT-IR infrared spectrometer), and the IR analysis and detection results are shown in Table 1.

[0023] Table 1 IR measurement data and analysis results...

Embodiment 2

[0027] Add 13.0g of propofol phosphate disodium salt of the formula (III) into a 50ml one-mouth bottle, add 26ml of water and stir to dissolve at 50°C, add an appropriate amount of activated carbon to decolorize for 15 minutes after complete dissolution, filter, and add the filtrate to 300ml iso In propanol, heat to reflux, stir to room temperature, place in the freezer and refrigerate until the crystallization is complete. Filtrate, wash, and dry to obtain 13.2 g of white crystals of propofol phosphate disodium salt hydrate, which was dried at 105° C. to constant weight. The measured water content was 21%, and the yield was 80.2%. The results of IR analysis are shown in Table 2.

[0028] Table 2 IR measurement data and analysis results

[0029]

Embodiment 3

[0031] Add 13.0 g of propofol phosphate disodium salt of formula (III) (commercially purchased or prepared according to the current literature method) into a 50 ml single-mouth bottle, add 30 ml of water and stir to dissolve at 50 ° C, after complete dissolution, add an appropriate amount of activated carbon to decolorize for 15 minutes, Filtrate, add the filtrate to 400ml of N,N-dimethylformamide under stirring, heat to reflux, stir to room temperature and place in a freezer to refrigerate until the crystallization is complete. Filtrate, wash, and dry to obtain 12.3 g of white crystals of propofol phosphate disodium salt hydrate, which was dried at 105° C. to constant weight. The measured water content was 10%, and the yield was 85.2%.

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Abstract

The invention discloses a substituted phenol for methylal phosphate anesthetic and sedative drugs and a preparation method thereof. The medicinal compound is a 2,6-diisopropyl phenol methylal phosphate disodium salt hydrate the molecular structure of which comprises 1-10 crystal water. The preparation method comprises the following steps: completely dissolving the 2,6-diisopropyl phenol methylal phosphate disodium salt hydrate in water, adding water-soluble organic solvent, and separating the hydrate by crystallization to obtain the medical compound. The medical compound in the form of a hydrate is not easy to absorb moisture, has good stability and easily controlled quality, and satisfactorily solves the urgent problems that the moisture content in the existing phosphate disodium salt compound is difficult to be controlled and the quality standard of existing phosphate disodium salt compound is difficult to be established due to strong moisture absorption of the existing phosphate disodium salt compound.

Description

technical field [0001] The invention relates to a phenol-substituted methylal phosphate anesthetic and sedative medicinal compound and a preparation method thereof. Background technique [0002] 2,6-diisopropylphenol (propofol) of structure shown in formula (II) is a kind of commonly used medicinal compound with effects such as sedation, hypnosis, anesthesia, has been widely used in clinical anesthesia and ICU sedation etc. application. The compound is a derivative of alkylphenol, has high fat solubility, is oily at room temperature, and is insoluble in water. [0003] [0004] In 1977, Kay and Rolly reported for the first time that propofol of formula (II) was used for clinical trials of anesthesia induction. Its early clinical preparation is 1% 2,6-diisopropylphenol aqueous solution prepared with 16% polyoxyethyl castor oil solution (cremophor EL) as solubilizer. This preparation was eliminated due to some problems in clinical application. In 1983, it was changed to...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/09A61K31/661A61P23/00A61P25/20
Inventor 刘进张文胜郑虎翁玲玲李章万
Owner SICHUAN UNIV
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