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Study On Synthesis Of Salbutamol And Gabapentin

Posted on:2010-07-31Degree:MasterType:Thesis
Country:ChinaCandidate:J P YangFull Text:PDF
GTID:2121360275993956Subject:Physical chemistry
Abstract/Summary:PDF Full Text Request
We studied the synthesis of salbutamol in the first section. Salbutamol is a very important category of pharmaceutical intermediate and aβ2 receptor agonists which the action has been widely confirmed and has applied for a longer period, has become more effective in the treatment of asthma drugs.The mechanism,new clinical application and harmful reflection of salbutamolare reviewed. The synthetic routes and synthesis process of salbutamol are researched particularly The parts are included as follows:We compare all the routes of the synthesis of salbutamol a great deal of literature. After thinking about the economic benefit,the environment problems and the feasibility in chemical production, o-dihydroxyacetophenone was used as the starting material to synthesize salbutamol by chloromethylation, sterification ,bromide, aminolysis,hydrolysis,reduction and the target compound was obtained .We studied the ratio of raw materials,the reaction process of feeding methods, the temperature and the time,find a series of after treatment of reactions which suitable for industrial production, Solved difficult problems of many impurities in the reaction of chloromethylation and can't attains the product in the ammonolysis response.We studied the synthesis of gabapentin in the second section. Gabapentin is an artificial amino acid which intuoduced to the market by Warner-Lambert. It is a good anti-epileptic drugs.Pharmacology, pharmacokinetics and of gabapentin were discussed briefly in the paper.The synthetic routes and synthesis process of gabapentin are researched particul-arly.The parts are included as follows:1 .We compare all the routes of the synthesis of gabapentinin a great deal of literature.cyclohexanone and Ethyl cyanoacetate were used as the starting material to synthesize Gabapentin hydrochloride by the reaction of Knoevenagel,Micheal addition, cyclization, aminolysis, decarboxylation, ammonolysis,Hoffman rearrangement.The target compound was obtained by PH adjusted with alkali to the isoelectric point of gabapentin.2.We optimized the synthesis process of gabapentinin,and have solved the problem of low yield in the reaction of hydrolysis and decarboxylation, make yield from 73% to 85%.3.Resolved the problem of from gabapentin hydrochloride obtained free amino acids,.through related references and tests.A final product stabilized with a yield of more than 90%.
Keywords/Search Tags:salbutamol, chloromethylation, industrial production, Gabapentin, Hydrolysis, decarboxylation
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