Synthesis method for Amantadine Hydrochloride

A technology of amantadine hydrochloride and its synthesis method, which is applied in the field of pharmaceuticals, can solve the problems of strong corrosion, expensive bromine, and difficult recovery, and achieve the effects of promoting isomerization reaction, increasing yield, and avoiding the generation of tar

Active Publication Date: 2011-05-11
GUIZHOU MAQIKA PHARMA
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  • Abstract
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Problems solved by technology

[0003] This synthesis process mainly reacts with urea through excess bromine and adamantane bromination. Not only is bromine more expensive and costly, but it is also highly corrosive, difficult to recycle, and seriously polluting.

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  • Synthesis method for Amantadine Hydrochloride

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Embodiment Construction

[0015] Example. The synthetic method of amantadine hydrochloride comprises the following steps, 1), hydrogenation: under the catalysis of nickel catalyst, dicyclopentadiene, hydrogenation reaction, control reaction pressure 1.5~1.8MPa, reaction temperature 110~155 ℃, early stage The temperature is 110-140°C. When the reaction does not absorb hydrogen, continue to heat and hold the pressure for 8 hours to obtain tetrahydrodicyclopentadiene; 2), isomerization and amination: according to the following weight ratio: tetrahydrodimerization 60 grams of cyclopentadiene, 20 grams of aluminum trichloride, and 120 milliliters of trichloroethane were reacted for 30 minutes at 30° C., wherein aluminum trichloride was the main catalyst and trichloroethane was the solvent, and then the temperature was slowly raised to 80 ℃, keep warm for 5 hours; when the temperature drops to about -10℃, start to add 10% nitrogen trichloride-trichloroethane solution dropwise, and keep the dropping temperatu...

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Abstract

The invention discloses a synthesis method for Amantadine Hydrochloride, which comprises the steps of hydrogenation, isomerization and amination, hydrolysis, refining, etc. to get Amantadine Hydrochloride finished product. Compared with the prior art, Trichloro ethane is adopted as solvent in the isomerization and amination steps, and bromination is cancelled, so that atmospheric pollution is lessened remarkably, and environmental pollution in the traditional process in Amantadine Hydrochloride synthesis is effectively solved. The invention has the advantages of no pollution, environmental friendliness, and better market application prospect.

Description

technical field [0001] The invention relates to a synthesis method of amantadine hydrochloride, which belongs to the technical field of medicines. Background technique [0002] Amantadine Hydrochloride (Amantadine Hydrochloride, 8-38) is a symmetrical tricyclic amine, which can inhibit the penetration of the virus into the host cell, and affect the uncoating of the virus and inhibit its reproduction. It has better treatment and prevention of viral infections role. At present, the general synthesis process of amantadine hydrochloride in China includes hydrogenation, isomerization, bromination, amination and refining processes, each process is: (1), hydrogenation: dicyclopentadiene is catalyzed by nickel catalyst , hydrogenation reaction, when the reaction pressure is controlled at 1.5-1.8MPa, the reaction temperature is 110-155°C, and the early stage temperature is 110-140°C. When the reaction does not absorb hydrogen, continue to heat and hold pressure for 8 hours to obtain...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C211/38C07C209/00
Inventor 张芝庭
Owner GUIZHOU MAQIKA PHARMA
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