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A kind of anesthetic suitable for brachial plexus anesthesia under the guidance of color ultrasound and its application

A technology of excipients and compounds, applied in the field of preparation of ropivacaine derivatives, can solve problems such as slow recovery of anesthesia consciousness

Active Publication Date: 2020-11-17
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current method to solve the above problems is mainly to add auxiliary drugs to ropivacaine as a local anesthetic for peripheral nerve block, such as dexamethasone, dezocine, etc. This method can effectively enhance the anesthesia effect and prolong the failure of anesthesia pain But sometimes there is a problem that patients recover slowly after anesthesia

Method used

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  • A kind of anesthetic suitable for brachial plexus anesthesia under the guidance of color ultrasound and its application
  • A kind of anesthetic suitable for brachial plexus anesthesia under the guidance of color ultrasound and its application
  • A kind of anesthetic suitable for brachial plexus anesthesia under the guidance of color ultrasound and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Preparation of N-cyclopropyl-2,6-dimethylaniline

[0027] Take 10g of 2,6-dimethylaniline and 2.1g of potassium carbonate into the ethanol solution, add bromopropane (calculated as 2,6-dimethylaniline, 1.05 equivalent) dropwise while stirring, and react under reflux for 4 hours. High performance liquid chromatography showed that the product's reduced pressure raw material 2,6-dimethylaniline was completely consumed, the reaction was stopped, and the solvent was removed by vacuum distillation to obtain 12.51g of yellow oily liquid, namely N-cyclopropyl-2,6-dimethyl Aniline, yield: 94%, ES-MS m / z 162[M+H + ].

Embodiment 2

[0028] Example 2: Preparation of compound I-1 (R=n-propyl)

[0029] Dissolve 4.5g of L-piperidine-2-carboxylic acid in 55mL of acetonitrile, slowly pass in HCl gas under stirring at room temperature until the pH of the reaction solution is 2~4, heat to 55℃, at this temperature, add 0.1mL of DMF, continue 3.8 g of thionyl chloride was dropped, and after the dropping was completed, the reaction was continued at this temperature for 2 hours. Continue to drip 8.6g of N-cyclopropyl-2,6-dimethylaniline in acetonitrile solution 15mL into the reaction solution, control the temperature of the reaction solution at 55~70℃, after reacting for 4 hours, add 5.6g of bromopropane , Add 3.2g potassium carbonate, react at 55°C for 6 hours, filter, and place the filtrate at 0°C to crystallize. Filtration, suction, and vacuum drying to obtain 6.9 g of light yellow solid. The crude product was hot-dissolved in toluene solvent at 60-80°C, filtered, cooled and crystallized and filtered to obtain 6.1 ...

Embodiment 3

[0031] Example 3: Preparation of compound I-2 (R=ethyl)

[0032] Dissolve 5.2 g of L-piperidine-2-carboxylic acid in 55 mL of dichloroethane, slowly pass in HCl gas under stirring at room temperature until the pH of the reaction solution is 2 to 4, heat to 55°C, add 0.1 mL of DMF at this temperature Then, 4.1 g of thionyl chloride was continuously added dropwise, and after the dropwise addition was completed, the reaction was continued at this temperature for 2.5 hours. Add 9.2g of N-cyclopropyl-2,6-dimethylaniline in 20mL of acetonitrile solution dropwise to the reaction solution. Control the temperature of the reaction solution at 55~70℃. After reacting for 4 hours, add 5.2g of ethyl bromide. Add 3.9 g of potassium carbonate, react at 40°C for 5 hours, filter, and place the filtrate at 0°C for crystallization. Filtration, suction, and vacuum drying to obtain 5.7 g of light yellow solid. The crude product was hot-dissolved in toluene solvent at 60-80°C, filtered, cooled and cr...

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Abstract

The invention provides an anesthetic, which is a compound of the formula I (please see the specification for the formula) or a pharmaceutically acceptable salt thereof, wherein R is C1-C5alkyl, preferably, R is ethyl, and propyl; the compound is used for color ultrasound-guided anesthesia of brachial plexus, when a small dose is injected to a patient, a good anesthesia blocking effect is brought,the effect is fast, blocking time is long, and the side effect is small.

Description

Technical field [0001] The invention relates to an anesthetic, in particular to an anesthetic suitable for anesthetizing the brachial plexus under the guidance of color Doppler ultrasound. More specifically, the invention relates to a derivative of ropivacaine, a preparation method and application thereof. Background technique [0002] With the development and progress of modern medicine, influence studies are more applied in surgical procedures. Color Doppler ultrasound guidance is accompanied by preoperative anesthesia, which greatly increases the safety of the operation. Intermuscular sulcus brachial plexus block is one of the commonly used anesthesia methods for upper limb surgery. In recent years, the application of high-frequency ultrasound guidance technology in brachial plexus block has gradually attracted attention. Compared with the traditional blind brachial plexus block for location of abnormal sense, ultrasound-guided inferior brachial plexus block has visibility, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/445A61P23/02
CPCA61K31/445A61P23/02
Inventor 周佳曾婷周杨胡春欢陈昕李冬梅
Owner MUDANJIANG MEDICAL UNIV
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