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Method for preparing lidocaine

A technology of lidocaine and dimethylaniline, applied in the field of anesthetic synthesis, can solve the problems of adverse environmental impact, high cost, low yield and the like, and achieves the effects of being environmentally friendly, avoiding loss and high yield

Active Publication Date: 2011-05-25
BENGBU BBCA MEDICINE SCI DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] But, the yield of above-mentioned traditional method is lower, and cost is higher, and the toluene used in the reaction process can cause bad influence to environment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1 two-step method prepares lidocaine

[0021] 1) Preparation of intermediate chloroacetyl-2,6-dimethylaniline

[0022] Add 102g of 2,6-dimethylaniline into a 1000mL three-necked flask, use 400mL of acetone as a solvent, then add 200g of potassium carbonate, stir mechanically and add 100mL of chloroacetyl chloride dropwise (1.5h to complete), at room temperature (20°C ) stirring reaction for 3h; suction filtration after the reaction, the filter cake was washed with water until the filtrate was neutral, and then dried at 100°C for 1 hour to obtain 156g of white powder, which was the intermediate chloroacetyl-2,6-dimethyl Aniline with a yield of 94% and a melting point of 145.0-147.0°C.

[0023] 2) Preparation of lidocaine

[0024] Add 80g of intermediate chloroacetyl-2,6-dimethylaniline into a 1000mL three-necked flask, use 400mL of acetone as solvent, add 112g of potassium carbonate after dissolving, quickly drop 60g of diethylamine, and reflux for 8 hours; ...

Embodiment 2

[0025] Embodiment 2 two-step method prepares lidocaine

[0026] 1) Preparation of intermediate chloroacetyl-2,6-dimethylaniline

[0027] Add 102g of 2,6-dimethylaniline to a 1000mL three-necked flask, use 400mL of acetone as a solvent, then add 163g of potassium carbonate, mechanically stir evenly, then add 80mL of chloroacetyl chloride dropwise (1.5h to finish), at room temperature (20°C ) stirring reaction for 3h; suction filtration after the reaction, the filter cake was washed with water until the filtrate was neutral, and then dried at 100°C for 1 hour to obtain 136g of white powder, which was the intermediate chloroacetyl-2,6-dimethyl Aniline with a yield of 82% and a melting point of 145-146°C.

[0028] 2) Preparation of lidocaine

[0029] Add 80g of intermediate chloroacetyl-2,6-dimethylaniline into a 1000mL three-necked flask, use 400mL of acetone as solvent, add 90g of potassium carbonate after dissolving, quickly drop 45g of diethylamine, and reflux for 8 hours; ...

Embodiment 3

[0030] Embodiment 3 two-step method prepares lidocaine

[0031] 1) Preparation of intermediate chloroacetyl-2,6-dimethylaniline

[0032] Add 102g of 2,6-dimethylaniline into a 1000mL three-necked flask, use 400mL of acetone as a solvent, then add 250g of potassium carbonate, stir mechanically and add 113mL of chloroacetyl chloride dropwise (1.5h to complete), at room temperature (20°C ) stirring reaction for 3h; suction filtration after the reaction, the filter cake was washed with water until the filtrate was neutral, and then dried at 100°C for 1 hour to obtain 150g of white powder, which was the intermediate chloroacetyl-2,6-dimethyl Aniline with a yield of 90% and a melting point of 147-148°C.

[0033] 2) Preparation of lidocaine

[0034] Add 80g of intermediate chloroacetyl-2,6-dimethylaniline into a 1000mL three-necked flask, use 400mL of acetone as a solvent, add 150g of potassium carbonate after dissolving, quickly drop 75g of diethylamine, and reflux for 8 hours; F...

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Abstract

The invention provides a method for preparing lidocaine. The method comprises the following steps: using 2,6-dimethylaniline and chloroacetic chloride as raw materials to prepare an intermediate, namely acetyl chloride-2,6-dimethylaniline, and using the prepared intermediate and diethylamine to react and obtain lidocaine, wherein acetone is used as solvent and carbonate is used as catalyst in thereaction process. The method of the invention has simple synthetic technology and does not require the complicated step that the intermediate is washed with acid firstly and washed with base secondlyin the post-treatment, thus avoiding unnecessary loss. Therefore, the yields of the intermediate and lidocaine prepared by the method are higher; and the prepared lidocaine has high purity which is more than 99%, and good industrial application prospect. In addition, the method of the invention uses acetone as solvent, thus the solvent is non-toxic basically and environmentally friendly, has no stimulation and can be recycled.

Description

technical field [0001] The invention relates to the technical field of synthesis of anesthetics, in particular to a method for preparing lidocaine. Background technique [0002] In recent years, although new anesthetics emerge in an endless stream, and dosage forms are also changing, the safest anesthetics are still old drugs that have been used for many years. The side effects of these old drugs have been known and mastered by people in many years of clinical practice, and the safety in actual use is higher than that of similar new drugs. [0003] Lidocaine is an anesthetic that has been clinically used for many years. It was first synthesized by Lofgren in 1934 and used as a local anesthetic. In the 1950s, it was used to treat ventricular arrhythmias that occurred during surgery. Because this drug has the advantages of being safe and effective, acting quickly, and disappearing quickly, it has been widely used to treat ventricular arrhythmia caused by various reasons. In...

Claims

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Application Information

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IPC IPC(8): C07C237/04C07C231/12
Inventor 胡媛郑爱张亚陈文婕赵辉戴荣欢
Owner BENGBU BBCA MEDICINE SCI DEV
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