Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Production method and application of lidocaine hydrochloride

A technology for lidocaine hydrochloride and a production method, which is applied in chemical instruments and methods, preparation of carboxylic acid amides, preparation of organic compounds, etc., can solve the problems of no curative effect, adverse reactions, and excessive carcinogen isopropylidene ketone. , to achieve the effect of reducing the incidence and improving product quality

Pending Publication Date: 2021-02-19
山东华鲁制药有限公司
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] After research by the inventors, it was found that the lidocaine hydrochloride prepared by the currently disclosed lidocaine hydrochloride production technology has the problem of many impurities. The impurities brought in during the production process not only have no curative effect, but may also cause adverse reactions. The carcinogen isopropyl ketone exceeded the standard, which brought risks to the patients who used it

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Production method and application of lidocaine hydrochloride
  • Production method and application of lidocaine hydrochloride
  • Production method and application of lidocaine hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Acylation reaction

[0049] 2,6-Dimethylaniline (kg): Chloroacetyl chloride (kg): Toluene (kg) = 1: 1.25: 5

[0050] Add toluene and 2,6-dimethylaniline into the reaction tank. Chloroacetyl chloride was added dropwise at 10°C for 1 hour. After the drop was completed, it took 2 hours to raise the temperature to boiling; slowly add 2,6-dimethylaniline 1 times purified water dropwise. The lower aqueous acid layer was discarded. Then use 2wt% potassium carbonate solution to neutralize the remaining acid, test the pH of the water layer to be greater than 7, and let off the water layer. Lower the temperature, drop the temperature of the feed liquid to room temperature, and centrifugally filter to obtain white needle-like crystals, ie, chloroacetylate.

[0051] condensation reaction

[0052] Chloroacetylate (kg): diethylamine (kg): toluene (kg) = 1:0.6:11

[0053] Pump the toluene into the condensation tank, put in the chloroacetylate, suck in the diethylamine, start stirri...

Embodiment 2

[0076] Acylation reaction

[0077] 2,6-Dimethylaniline (kg): Chloroacetyl chloride (kg): Toluene (kg) = 1:1:7

[0078] Add toluene and 2,6-dimethylaniline into the reaction tank. Chloroacetyl chloride was added dropwise at 20 o'clock for 1 hour. After the drop, it took 5 hours to raise the temperature to boiling; slowly add 2,6-dimethylaniline 2 times purified water dropwise. The lower aqueous acid layer was discarded. Then use 3wt% potassium carbonate solution to neutralize the remaining acid, test the pH of the water layer to be greater than 7, and let off the water layer. Lower the temperature, drop the temperature of the feed solution to room temperature, and centrifugally filter to obtain white needle-like crystals, namely chloroacetylated compounds.

[0079] condensation reaction

[0080] Chloroacetylate (kg): diethylamine (kg): toluene (kg) = 1:1:8

[0081] Pump the toluene into the condensation tank, put in the chloroacetylate, suck in the diethylamine, start stir...

Embodiment 3

[0101] Acylation reaction

[0102] 2,6-Dimethylaniline (kg): Chloroacetyl chloride (kg): Toluene (kg) = 1:1.5:12

[0103] Add toluene and 2,6-dimethylaniline into the reaction tank. Chloroacetyl chloride was added dropwise at 50°C for 1 hour. After the drop, it took 7 hours to raise the temperature to boiling; slowly add 2,6-dimethylaniline 5 times purified water dropwise. The lower aqueous acid layer was discarded. Then use 5wt% potassium carbonate solution to neutralize the remaining acid, test the pH of the water layer to be greater than 7, and let off the water layer. Lower the temperature, drop the temperature of the feed solution to room temperature, and centrifugally filter to obtain white needle-like crystals, namely chloroacetylated compounds.

[0104] condensation reaction

[0105] Chloroacetylate (kg): diethylamine (kg): toluene (kg) = 1:1.5:5

[0106] Pump the toluene into the condensation tank, put in the chloroacetylate, suck in the diethylamine, start stirr...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a production method and application of lidocaine hydrochloride, wherein the production method comprises the steps: carrying out acylation reaction on 2,6-dimethylaniline and chloroacetyl chloride to obtain a chloroacetyl compound, carrying out condensation reaction on the chloroacetyl compound and diethylamine to obtain lidocaine, and reacting lidocaine with hydrogen chloride gas to obtain a lidocaine hydrochloride crude product; refining the lidocaine hydrochloride crude product to obtain lidocaine hydrochloride, wherein solvents adopted in the acylation reaction and the condensation reaction are toluene, solvents of lidocaine and hydrogen chloride gas are acetone, and a refined solvent system is acetone and water; and after the condensation reaction, extracting the material with an acid solution, adding activated carbon for adsorption, filtering to remove the activated carbon, and adding an alkaline solution for treatment to obtain lidocaine. According to themethod, impurities of lidocaine hydrochloride can be greatly reduced, so that the safety and effectiveness of the lidocaine hydrochloride product are improved.

Description

technical field [0001] The invention relates to a production method and application of lidocaine hydrochloride. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Lidocaine hydrochloride is an amide local anesthetic. After blood absorption or intravenous administration, it has obvious excitatory and inhibitory biphasic effects on the central nervous system, and there may be no precursor excitement. When the blood concentration is low, analgesia, drowsiness, and pain threshold increase. Large, enhanced effect or toxicity, anticonvulsant effect at subtoxic blood concentration. Since lidocaine hydrochloride is mainly administered through intramuscular injection or intravenous...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07C231/12C07C237/04
CPCC07C231/12C07C231/02C07C237/04C07C233/13
Inventor 于洪华张艳梅赫明凯韩丽云于睿思崔俊德郑风武颜景洋李文建
Owner 山东华鲁制药有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com