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Compound applicable to anesthetics

A technology of anesthetics, organic compounds, applied in the field of medicinal chemistry

Inactive Publication Date: 2014-06-04
李飞燕
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There are many kinds of anesthetics in the prior art, but these anesthetics all have different degrees of side effects, and it is still necessary to develop compounds that are effective and have no side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0020] The raw material compounds were purchased from ACROS ORGANICS, and the solvents and reagents were commercially available analytical reagents.

Embodiment 1

[0021] Embodiment 1, the synthesis of formula I compound:

[0022] (1) Synthesis of (E)-4-(2-hydroxyphenyl)-3-buten-2-one

[0023] Add 2-hydroxybenzaldehyde (20.0 mmol), 24 mL of acetone, and 10 mL of water to a 100 mL three-necked flask in sequence, stir at room temperature until all solids are dissolved, then add a solution of sodium hydroxide (24 mmol) + 20 mL of water drop by drop , the reaction liquid changed from light yellow clear liquid to wine red clear liquid, the reaction was complete, acetone was removed by rotary evaporation, 70 mL of hot water was added to the residual liquid until the red solid was completely dissolved, carbon dioxide was introduced for about 30 min until the reaction liquid no longer changed color So far, a light yellow solid is produced, filtered, washed with water, dried, and recrystallized with acetone / water to obtain a light yellow solid with a yield of 78.3% and a melting point of 137~139 °C.

[0024] (2) Synthesis of (1E,4E)-1-(2-hydroxy...

preparation Embodiment 2

[0035] The compound of formula I was placed in a quartz ampoule. The prepared compound was vacuum dehydrated at a temperature of 100°C. The tube was disengaged and placed in a crystal growth furnace. Crystals were grown by the Bridgman method in a double furnace with an insulating film. Finally, colorless needle-like crystals were obtained. The crystal is subjected to single crystal X-ray diffraction crystallographic analysis, and its crystallographic parameters are as follows: it is an orthorhombic system, and its space group is P2 1 , a=7.81 ?, b=6.54 ?, c=3.21 ?, β=89.5°, V=163.96 ? 3 .

[0036] Biologically active examples:

[0037] The in vitro efficacy [inhibition of the compound of embodiment 1 and the compound of embodiment 2 is compared in table 1 35 S]-Binding ability of tert-butylbicyclic glucothioate (TBPS)], rotating rod TD 50 (dose at which half of the test animals cannot stay on the rotating rod for 1 minute) and the length of time before all test anima...

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Abstract

The invention provides an organic compound applicable to anesthetics, which can be used as a sedative / hypnotic and for anesthetization.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry and methods and methods of organic compounds for regulating brain stimulation. Background technique [0002] Anesthetics refer to drugs that can cause temporary and reversible loss of consciousness and pain in the whole body or parts of the body. According to its scope of action, it can be divided into general anesthetics and local anesthetics. General anesthetics and local anesthetics can be divided into inhalational anesthetics and intravenous anesthetics according to their different action characteristics and administration methods. Local anesthesia can be used, and the effect is very good. [0003] Anesthetics are divided into general anesthetics and local anesthetics. General anesthetics inhibit the cerebral cortex from shallow to deep, making people lose their consciousness. Local anesthesia can stabilize the membrane potential of the nerve or reduce the permeability of the memb...

Claims

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Application Information

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IPC IPC(8): C07D213/61A61K31/44A61P23/00A61P25/20
CPCC07D213/61
Inventor 李飞燕
Owner 李飞燕
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