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Short-acting hypnotizing and calming compound used for anesthetization

A compound and alkyl technology, applied in the directions of active ingredients of heterocyclic compounds, anesthetics, organic chemistry, etc., can solve the problems of poor efficacy and insufficient anesthetic effect, and achieve low toxicity and side effects, predictable recovery time, and strong anesthetic activity. Effect

Active Publication Date: 2010-04-28
李世系
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the anesthetic effect of this type of compound is not strong enough, and the drug effect is relatively poor, which cannot meet the current medical needs.

Method used

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  • Short-acting hypnotizing and calming compound used for anesthetization
  • Short-acting hypnotizing and calming compound used for anesthetization
  • Short-acting hypnotizing and calming compound used for anesthetization

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] 1.1, the synthetic technique of (3-trifluoromethoxy-4-hydroxyl) n-propyl phenylacetate (compound a):

[0078]

[0079] Compound a can be prepared by the following reaction scheme:

[0080]

[0081] 1.1.1 Compound a 1 The synthesis process:

[0082] Add 35.6g of 2-trifluoromethoxyphenol, 37ml of glyoxylic acid (40%), and 60ml of purified water into a 500ml three-necked flask equipped with mechanical stirring and a thermometer, cool in an ice bath to below 10°C, and slowly add 10 % sodium hydroxide solution 160ml, and maintain this temperature, add sodium hydroxide solution, temperature rises slowly to room temperature, maintain room temperature reaction 20 hours. The solution was extracted with 2×50ml ethyl acetate, then adjusted to pH 3 with concentrated hydrochloric acid, saturated with NaCl, extracted with 3×100ml ethyl acetate, the ethyl acetate layer was washed with 3×100ml saturated brine, anhydrous MgSO 4 Dry overnight, evaporate the solvent under reduced...

Embodiment 2

[0103] 2.1, Synthetic process of [3-(1.1.2.2-tetrafluoroethoxy)-4-hydroxy]n-propyl phenylacetate (compound b):

[0104]

[0105] 2.1.1 Compound b 1 The synthesis process:

[0106]

[0107] Using 2-(1.1.2.2-tetrafluoroethoxy)phenol instead of 2-trifluoromethoxyphenol, it was prepared using a similar process as described in Example 1.1.1. With 2-(1.1.2.2-tetrafluoroethoxy)phenol 42g, compound b was obtained 1 39.5g.

[0108] Elemental analysis result: C 10 h 8 f 4 o 5 C 42.25 H 2.82

[0109] Mass Spectrometry Results: M / Z[M+H + ]284

[0110] 2.1.2 Compound b 2 The synthesis process:

[0111]

[0112] It was prepared using a similar process as described in Example 1.1.2. Compound b from the previous step 1 28.5g, to obtain compound b 2 30.5g.

[0113] Elemental analysis result: C 14 h 12 f 4 o 7 C 45.65 H 3.27

[0114] Mass Spectrometry Results: M / Z[M+H + ]368

[0115] 2.1.3 Compound b 3 The synthesis process:

[0116]

[0117] It was prepa...

Embodiment 3

[0130] 3.1, the synthetic technique of [3-(2.2.2-trifluoroethoxy)-4-hydroxy]n-propyl phenylacetate (compound c):

[0131]

[0132] 3.1.1 Compound c 1 The synthesis process:

[0133]

[0134] It was prepared by a similar process described in Example 1.1.1 by substituting 2-(2.2.2-trifluoroethoxy)phenol for 2-trifluoromethoxyphenol. With 2-(2.2.2-trifluoroethoxy)phenol 38.5g, compound c was obtained 1 34g.

[0135] Elemental analysis result: C 10 h 9 f 3 o 5 C 45.10 H 3.40

[0136] Mass Spectrometry Results: M / Z[M+H + ]266

[0137] 3.1.2 Compound c 2 The synthesis process:

[0138]

[0139] It was prepared using a similar process as described in Example 1.1.2. Compound c from the previous step 1 26.6g, to obtain compound c 2 25.5g.

[0140] Elemental analysis result: C 14 h 13 f 3 o 7 C 47.99 H 3.73

[0141] Mass Spectrometry Results: M / Z[M+H + ]350

[0142] 3.1.3 Compound c 3 The synthesis process:

[0143]

[0144] It was prepared using ...

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Abstract

The invention discloses a phenyl acetic vinegar compound shown in the general formula (I), wherein A represents CnHmFxClyBrz and at least has an alkyl group, a naphthenic group, an olefine group or an alkyne group which is substituted by a halogen atom; n in the A is 1-6, m is 0-2n, x is 0-2n, y is 0-2n, z is 0-2n, m+x+y+z=2n+1, 2n-1 or 2n-3, and x+y+z >= 1; and R1, R2 and R3 represent alkyl groups of C1-C6, olefine groups of C2-C6 or alkyne of C2-C6 which are respectively independent. The invention also relates to a medicine composition taking the compound as an active component and the application of the compound and the medicinal composition in an anesthetization maintaining, inducement and hypnotizing calmative of people or animals.

Description

technical field [0001] The present invention relates to a substituted phenylacetate compound, which can be used as short-acting anesthesia maintenance, anesthesia induction and sedation for humans or mammals, and a pharmaceutical composition containing this compound. Background technique [0002] When performing general anesthesia on humans or animals, an ideal anesthetic should have a short onset time, strong depth of anesthesia, predictable duration of anesthesia, and less toxic side effects. There are currently two types of general anesthetic drugs that are clinically popular: [0003] Propofol, namely 2,6-diisopropylphenol (Diprivan. Injectable Emulsion, AstraZeneca) is an injectable anesthetic with hypnotic properties. It can be used to induce and maintain general anesthesia and sedation, with quick onset, deep anesthesia intensity, and less toxic and side effects. Although propofol is a widely used anesthetic, its usefulness is limited by its long and unpredictable d...

Claims

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Application Information

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IPC IPC(8): C07C235/20C07D295/185A61K31/165A61K31/40A61P23/00A61P25/20
Inventor 刘红旗李世系
Owner 李世系
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