含異噁唑的甘草次酸酰胺衍生物和莫吉司坦的合成研究.pdf

1、天津大學(xué)碩士學(xué)位論文含異噁唑的甘草次酸酰胺衍生物和莫吉司坦的合成研究姓名：甘英健申請學(xué)位級別：碩士專業(yè)：制藥工程指導(dǎo)教師：黃耀東羅振福20090501ABSTRACTThispaperwasaboutthesynthesisresearchofmainlyanti—inflammatorydrugswithisoxazoleofglycyrrhetinicacidamidecompoundsandofsuppressantsMoggis

2、tanozol01Containingisoxazoleglycyrrhetinicacidamideofthesyntheticcompoundstoochlorobenzaldehydeasstartingmaterial，throughoxime，cycloaddition，bromide，ammoniasolution，andacylationtosynthesisofthefinalproduct，andstudieditsk

3、eystepsInthesynthesisprocess，therawmaterialsandreagentsusedarecommon，readilyavailablePreparationofthealdehydeoxime，withtriethylamineasacidbindingagentinsteadofNa2C03andmethanolassolventintheprocessofsynthesishydroxymethy

4、l—isoxazoleuseNa2C03insteadoftriethylamineasacatalyst，andvolumeratio2：1ofetherandtolueneasacrystallizationsolvent，theyieldhasimprovedmarkedlyInthepreparationprocessofbromomethylisoxazole，useofpyridineascatalystmethylbrom

5、ideandthreebromidelsoxazolephosphOruSmolarratioof1：115InthepreparationprocessofSMZamine，thebromomethylisoxazoleurotropineandthemolarratioof1：11alkylationtimeforsixhoursismosttimelySynthesisoftargetedproducts，thereactiont

6、imeof24hourscanhavethehighestyield，witha，totalyieldof4575％Inmoguisteinesynthesis，guaiacolWaSinitialmaterialandmoguisteinewassynthezedbysubstitution，cyclization，NacylationandSOon，accordingteferenceAndsyntheticalstepswasim

7、proved：DMFwhichwaslowcostandharmfullesssubstitudedNMPasreactionreagentforsubstitution，andreactiontimewasprolongedto85hForcyclization，orthogonaltestwasusedforensuringtheoptimalconditionsofreaction：reactiontimewas4h，reacti

8、onreagentwasethanolandwaterofwhichratiobyvolumewas1：1，thetoolratioof2(2methoxyphenoxy)acetaldehydediethyacetalandcysteaminehydrochloridewas1：150N—acylationappliedtriethylamineasacidacceptertomakereactionsystemhomogeneous