Anesthetic for color ultrasound-guided anesthesia of brachial plexus and application of anesthetic

A reaction and acid-binding agent technology, applied in the field of preparation of ropivacaine derivatives, can solve problems such as slow recovery of anesthesia consciousness

Active Publication Date: 2019-10-29
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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  • Anesthetic for color ultrasound-guided anesthesia of brachial plexus and application of anesthetic
  • Anesthetic for color ultrasound-guided anesthesia of brachial plexus and application of anesthetic
  • Anesthetic for color ultrasound-guided anesthesia of brachial plexus and application of anesthetic

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation of N-cyclopropyl-2,6-dimethylaniline

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

Embodiment 2

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

[0029] Dissolve 4.5g of L-piperidine-2-carboxylic acid in 55mL of acetonitrile, slowly inject HCl gas under stirring at room temperature until the pH of the reaction solution is 2-4, heat up to 55°C, at this temperature, add 0.1mL of DMF, continue 3.8 g of thionyl chloride was added dropwise, and after the dropwise addition was completed, the reaction was continued at this temperature for 2 hours. Continue to drop 15mL of 8.6g of N-cyclopropyl-2,6-dimethylaniline in acetonitrile solution to the reaction solution, control the temperature of the reaction solution at 55-70°C, after 4 hours of reaction, add 5.6g of bromopropane , add 3.2g of potassium carbonate, react at 55°C for 6 hours, filter, and place the filtrate at 0°C for crystallization. Filtration, vacuum drying, and vacuum drying yielded 6.9 g of a light yellow solid. The crude product was hot-dissolved in toluene solvent at 60-80°C, filtered, cooled, cry...

Embodiment 3

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

[0032] Dissolve 5.2g of L-piperidine-2-carboxylic acid in 55mL of dichloroethane, slowly inject HCl gas under stirring at room temperature until the pH of the reaction solution is 2~4, heat up to 55°C, at this temperature, add 0.1mL of DMF Afterwards, continue to dropwise add 4.1g of thionyl chloride, and after the dropwise addition is completed, continue to react at this temperature for 2.5 hours. Continue to drop 20 mL of acetonitrile solution of 9.2 g of N-cyclopropyl-2,6-dimethylaniline into the reaction solution, control the temperature of the reaction liquid at 55-70 °C, and after 4 hours of reaction, add 5.2 g of ethyl bromide alkane, add 3.9g of potassium carbonate, react at 40°C for 5 hours, filter, and crystallize the filtrate at 0°C. Filtration, vacuum drying, and 5.7 g of a light yellow solid were obtained. The crude product was dissolved in toluene solvent at 60-80°C, filtered, cooled, crystallized and...

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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 present invention relates to an anesthetic, in particular to an anesthetic suitable for anesthesizing the brachial plexus under the guidance of color ultrasound, more specifically, the present 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 used in the operation process. Color Doppler ultrasound guidance accompanied by preoperative anesthesia greatly increases the safety of the operation. Interscalene brachial plexus block is one of the commonly used anesthesia methods for upper extremity surgery. In recent years, the application of high-frequency ultrasound-guided technology in brachial plexus block has gradually attracted attention. Compared with the traditional paraesthesia localization blind piercing brachial plexus block, ultrasound-guided brachial plexus block has visibility, can clea...

Claims

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Application Information

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Patent Type & Authority Applications(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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