Production of benzyl lidocaine halogenated amine

A benzyl lidocaine ammonium halide, production method technology, applied in chemical instruments and methods, preparation of organic compounds, organic chemistry and other directions, can solve problems such as high production cost, large solvent consumption, etc., achieve short reaction time, solvent Low dosage effect

Active Publication Date: 2007-06-20
浙江合糖科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In order to eliminate potential safety hazards in the production process of benzyl lidocaine ammonium halide and overcome the defe

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0014] Example 1

[0015] Add 400Kg lidocaine and 240Kg benzyl chloride into a 1000L reaction kettle, then add 300Kg cyclohexane, heat to reflux with stirring for 12 hours, then cool to room temperature, filter, wash the solid with appropriate amount of cyclohexane, and dry to obtain 530Kg Benzyl lidocaine ammonium chloride, the yield is 86.0%, and the content is 99.3%. The mother liquor obtained by filtration and the washing liquor are combined.

Example Embodiment

[0016] Example 2

[0017] Add 400Kg lidocaine and 240Kg benzyl chloride into a 1000L reaction kettle, then add the mother liquor and washing liquid combined in Example 1, and other operating conditions are the same as in Example 1, to obtain 561Kg of benzyl lidocaine ammonium chloride, yield 91.0%, the content is 99.4%.

Example Embodiment

[0018] Example 3

[0019] Add 400Kg lidocaine and 250Kg benzyl chloride into a 1000L reactor, then add 300Kg of chlorobenzene, heat to reflux with stirring for 4 hours, then cool to room temperature, filter, wash the solid with an appropriate amount of chlorobenzene, and dry to obtain 521Kg of benzyl Lidocaine ammonium chloride has a yield of 84.5% and a content of 99.5%. The mother liquor obtained by filtration and the washing liquor are combined.

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PUM

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Abstract

Production of benzyl-lidocaine ammonium halide is carried out by reacting lidocaine with benzyl halide at 60-160degree in organic solvent, stopping reaction, cooling and crystallizing to obtain the final product. The organic solvent is selected from C5-C10 cyclanes, C6-C10 aryl halide and C4-C8 ketone. It has short reactive time and more solvent and can be used for large-scale industrial production.

Description

(1) Technical field [0001] The invention belongs to a production method of benzyl lidocaine ammonium halide. (2) Background technology [0002] In the 1960s, the United Kingdom and the United States applied for the application patent (T.E.Hag GB955309) of benzyl ammonium benzoate amide, which involved the synthesis method of the compound, that is, using an excess of benzyl halide and lidocaine to react at 110 ° C for 36 hours, and in the middle The product benzyl lidocaine ammonium halide reacts with methanol caustic potash after secondary recrystallization, filters the precipitate, and reacts with benzoic acid to obtain the crude product (solid) of benzyl ammonium benzoate amide with a melting point of 155-157°C. In 1998, the Institute of Chemical Metallurgy, Chinese Academy of Sciences applied for a patent for its synthesis method (ZL98100785.6), which mentioned that benzyl halide and lidocaine were reacted at 50-105°C for 10-30 hours, and the intermediate benzyl halide wa...

Claims

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Application Information

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IPC IPC(8): C07C231/12C07C237/20
Inventor 姜国平严晓阳
Owner 浙江合糖科技有限公司
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