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Method for synthesizing doxylamine succinate

A technology for the synthesis of doxylamine succinate and its synthesis method, which is applied in the field of synthesis of ethanol antihistamines and can solve the problems of no literature reports on doxylamine succinate

Inactive Publication Date: 2011-06-29
HEFEI UNIV OF TECH +1
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the synthesis technique of doxylamine succinate has no bibliographical information at home and abroad

Method used

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  • Method for synthesizing doxylamine succinate
  • Method for synthesizing doxylamine succinate
  • Method for synthesizing doxylamine succinate

Examples

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Embodiment Construction

[0033] 1. Synthesis of 2-pyridylphenylmethylcarbinol

[0034] Take 3.12g (0.13mol) of magnesium chips into a 250ml three-neck flask, add 50ml of anhydrous ether, stir, take 17.27g (0.11mol) of bromobenzene and mix 50ml of anhydrous ether, and slowly drop them. About 10 minutes to drip. After the reaction was initiated, a large amount of diethyl ether was refluxed, and the reaction solution became cloudy and the color gradually turned to metallic gray. Keep ether at reflux for two hours. Take 12.1g (0.1mol) of 2-acetylpyridine, mix with 30ml of anhydrous diethyl ether, and slowly add it dropwise to the above-mentioned Grignard reagent, and the dropping rate is controlled at 2 seconds per drop. When the mixture was added to Grignard reagent, it immediately turned into a white milky substance, and a large amount of heat was released, and anhydrous ether was refluxed. After the dropwise addition, the solution became clear, and a gray sticky substance appeared at the bottom of t...

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Abstract

The invention discloses a method for synthesizing doxylamine succinate. 2-acetylpyridine is taken as an initiative material, and the method comprises the following steps of: reacting the 2-acetylpyridine with a Grignard reagent prepared from bromobenzene and magnesium to obtain 2-pyridyl phenyl methyl carbinol; reacting the 2-pyridyl phenyl methyl carbinol with sodium amide and 2-dimethylaminoethyl chloride in turn to obtain doxylamine; and performing salt-forming reaction on the doxylamine and succinic acid to obtain the doxylamine succinate. The synthesis route is orientation reaction without byproduct. The doxylamine succinate is an ethanol antihistamine, and has antihistaminic and cholinolytic effects and obvious tranquillizing effect.

Description

1. Technical field [0001] The invention relates to a method for synthesizing ethanol antihistamines, in particular to a method for synthesizing doxylamine succinate. 2. Background technology [0002] Doxylamine succinate is an ethanol antihistamine with antihistamine, anticholinergic and significant sedative effects. It is suitable for a variety of allergic skin diseases, hay fever, allergic rhinitis, and asthmatic bronchitis etc.; it can also be used as a hypnotic for the short-term treatment of insomnia, which produces drowsiness by inhibiting the central nervous system. [0003] In October 1978, the FDA approved the marketing of doxylamine 25mg tablets of CHATTEM company, which is used to help alleviate the difficulty of falling asleep. Became OTC (over the counter) in 1979. It was approved in September 1996, and in August 2004, LNK was officially listed as a generic drug. Doxylamine, as an OTC antihistamine drug for adjuvant sleep therapy, is clinically safe and effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/30C07C55/10C07C51/41
Inventor 许华建齐洪侠王珏玉郑法银曹明成晏飞冯乙巳
Owner HEFEI UNIV OF TECH
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