抗癫痫药托吡酯的合成及工艺研究-制药工程专业毕业论文.docxVIP

AbstractEpilepsy Abstract Epilepsy is the most conllnon of the nervous system disease，the patient about 50 millions ill the global．and the treatment is still dominated by drugs at present．Before the appearance of the new antiepileptic drugs，the therapy method is mainly depends on the traditional one· But the limitations of the pharmacokinetics，the possibility of the teratogenicity,and the bad effect on cognitive functioning，which limit their applications．The invention of antiepileptic drugs and applications bring the epilepsy sufferers with hope and more choices· As a new type of antiepileptic drug,Topirarnate is the sulphur generation product of the natI】ra I state，D．fructos．It has the hi。gh bioavailability，long acting time and many obvious advantages．In addition，it has the multiple role of the mechanism，good effect on many types of epileptic in clinical treatment．Its tolerance and security are also good，and belongs to powerful and broad spectrum antiepileptic drug． On the basis of synthetic methods reported in literatures，the systematic study on the synthesis process was carded out，and the conditions of the key unit reaction in the synthesis were improved．This method avoids the using of highly toxic and corrosive materials，have the advantage of mild react conditions，easy operation，and security．All of that is appropriate for magnifying and industrial production．The structure of the Topiramate and its key intermediate products were characterized by element analysis，infrared analysis and melt point determinate． Main contents and The innovations： (1)The diacetonefructose Was obtained with D-fructose and acetone，and the concentrated sulphuric acid Was used as catalyzer．The possible effect factors to the yield of the product were also studied and the optimal inventory,reactor temperature and time were confirmed． (2)The chlorosulfate，a important intermediate product，prepared with sulfuric chloride and diacetonefructose．The dichloroethane Was replaced by dichlorometha