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Extraction Of Hyodeoxycholic And Synthesis Of And Ursodesoxycholic Acid And Its Deirvatives

Posted on:2015-10-31Degree:MasterType:Thesis
Country:ChinaCandidate:F ZhangFull Text:PDF
GTID:2284330467468978Subject:Microbial and Biochemical Pharmacy
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It has been more than thousands of years that the animal bile was used as drug inChina. With the development of science technology new drug research anddevelopment face more and more fierce competition and challenges in china andabroad and the focus of the new drug research increasingly turn to traditional Chinesemedicine and natural medicine Discovery and utilization of the active ingredient.Atpresent due to the synthesis of artificial bezoar and the emergence of a large numberof bile acid preparation,social demand for bile is Demand more and more, therefore,its manufacture method is particularly important,how to efficiently get cheap thesebile acid has been a focus in the study of relevant researcher,Due to China is already a long time for the comprehensive utilization of pig bileacid source, and the pig bile acid resources are rich. In This paper, purehyodeoxycholic acid and chenodeoxycholic acid separated from the mixed Pig bilepowder at one time with short steps, two individual components whose puritiesdetected by HPLC was beyond98%.The route,which could not only make the bestrecycle of raw material,is applicable to industrial production,In This paper,chenodeoxycholic acid and ursodeoxycholic acid was respectivelysynthesized from hyodeoxycholic acid, To optimize the synthetic process ofchenodeoxycholic acid and ursodeoxycholic acid,And to increase the yield,Grope forreaction conditions and recrystallization.The yields of these compounds had beenimproved. The overall yield of chenodeoxycholic acid and ursodeoxycholic acidrespectively reached to26%and19%. The target compounds are reportedcompounds,whose structure can be confirmed by melting point MS and1HNMR.Theimproved synthetic process has the advantages of easy availability of startingmaterials,highly stereoselectivity,easily work-up and good overall yield, so it hasconsiderable practical value.In this paper,in order to further find highly active, low toxicity and is easy to beabsorbed by human body.This paper took ursodeoxycholic acid as the lead compoundand got glycoursodeoxycholic acid derivatives.Then two series of compounds wereproduced by combining phenols and amines with the carboxyl group ofglycoursodeoxycholic acid.These13compounds had all been purified, confirmed by1HNMR and MS.This work will be helpful to the further research and development of ursodeoxycholic acid....
Keywords/Search Tags:hyodeoxycholic acid, chenodeoxycholic acid, ursodesoxycholic acid, derivative, synthesis
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