Synthesis process of amantadine

Physical and chemical properties
  Amantadine is also known as tricyclodecanamine. Slightly soluble in water, soluble in chloroform, melting point 180-192 °C (sealed). White crystalline powder, odorless and tasteless. Stable to light and air, soluble in 2.5 times water, soluble in 5 times ethanol, 18 times chloroform, insoluble in benzene and ether.
  In addition to the prevention and early treatment of Asian influenza A-11, it can also be combined with antibiotics to treat sepsis and viral pneumonia, and has fever-reducing effect. It also has an anti-tremor paralysis effect.
Amantadine production status
  China's amantadine was first developed and marketed by Northeast Pharmaceutical General Factory in 1971. At present, the main domestic manufacturers are Northeast Pharmaceutical General Factory, Zhejiang Kangyu Pharmaceutical, Zhejiang Dier Chemical, etc., of which Zhejiang Kangyu Pharmaceutical has an annual output of 300 tons, with a market share of about 45%.
Synthesis method
Synthesis method - synthesis of amantadine from bromoadamantane
The second synthesis method - amantadine synthesis by reducing nitro with zinc powder
A synthesis method - hydrazine hydrate reduction nitro method to synthesize amantadine
Method: The method of synthesizing amantadine from bromoadamantane is still the main process for the industrial production of amantadine, which can be seen in the industrial production line, at present, it has irreplaceable advantages. Therefore, on this basis, if the production process can be improved as much as possible, the amount of bromine can be reduced or other bromine-containing substances that can replace bromine can be found for halogenation reaction, so as to reduce environmental pollution as much as possible, if at the same time can provide better reaction selectivity and yield, it will produce better profits and promote the rapid development of amantadine production. As described in the above experiment, in the existing process, the full and uniform contact between adamantane and bromine as much as possible will facilitate the reaction with high selectivity and high yield, and if the boiling point of the solvent is too low in the reaction, the reaction will not be able to proceed. However, the yield of this reaction is not too high, and it is quite different from the other two methods.
The second method: the reduction of 1-nitroadamantane by zinc powder reduction method is relatively simple, the reaction speed is faster, and the yield is high, but the metal sludge produced will cause serious pollution.
The third method: hydrazine hydrate reduction method hydrazine hydrate is a carcinogen, which also has toxic and pollution problems.
By improving the second method, the amorphous alloy catalyst is used for hydroreduction reaction, which realizes multiple applications, reduces production costs, and the used waste catalyst can be recycled into other nickel compounds to achieve green environmental protection and pollution-free production, which is used by domestic manufacturers.



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