有机小分子催化的杂环化合物的合成研究

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1、东南大学博士学位论文有机小分子催化的杂环化合物的合成研究姓名：石春玲申请学位级别：博士专业：制药工程指导教师：吉民20090222中文摘要另外还具有一定的区域选择性等特点，具有重要的理论意义和应用价值。关键词：有机小分子；杂环化合物；L-脯氨酸；呋喃并吡啶并吡唑：双吡啶酮；吡喃并喹啉二酮；多组分一锅法Ⅲ英文摘要SynthesisResearchofheterocycliccompoundscatalyzedbysmallorganicmolecules(DissertationforPh．D．Degree)Candidate：SHIChunlingSu[Pro

2、f．JISuDervlsor：roMi。nMSchoolofChemistry&ChemicalEngineering，SoutheastUniversityABSTRACTOrganicsynthesiscatalyzedbysmallorganicmoleculesisrecentlyoneofhotspotsinorganicchemistry．Organiccatalysisisthereactionusingsmallorganicmoleculenotcontainingmetalasacatalystwithastoichiometry(orca

3、talyticamount)．Organiccatalystswitheasyoperationstilltakemanygreenadvantagesofenvironmentalfriendliness，lowcost,easymodi匆andpreparation,mildreactionconditions，operationalsimplicityandrecycle，atomeconomy，ota1．Inthisdissertation,itisoverviewedthatclassificationoforganiccatalystsandits

4、newapplicationprogressinorganicsynthesisaccordingtothedomesticandforeignliteratures．11heresearchofnewmany-componentreactions(MCRs)inthesynthesisofheterocyeliecomponentscatalyzedbysmallorganicmoleculesalefocusedoninordertoinvestigateandresearchapplicationofsmallorganicmoleculesinorga

5、nicsynthesis，andfindthemappliedtothesynthesisofmoreheterocycliccompounds诵廿1potentialbioactivitiesandpharmacologicalactivities．Thewholeworkismainlycomposedofthefollowingfourparts：PartI：P埘dinopyrazolinesa佗akindoffusedheteroeycliccompoundsresearchedextensivelywithimportantbioactivities

6、andpharmacologicalactivities，anddihydrofuropyridinopyrazolinesa他thecompoundswi缅potentiallymedicalvalue．Viaone-potMCRscatalyzedbyorganiccatalystsof5-amino-3-methyl-1-phenyipyrazoline，aldehydes，tetronicacid(or1,3一indanedione)，dihydrofuro[3',4’：5，6】pyridine[2，3-c]pyrazolineandindeno[2’

7、，1’：5，6]pyridine[2，3-c]pyrazolinederivativesaresynthesized．Thismethodtakesadvantagesofhighyields，easyoperation,recyclabilityandenvironmentalfriendliness．SomeofthenewproductshaveastrongerinhibitoryeffecttohumanlivercancercelllineHepG2，atmorethan80％ofinhibitionrate．PartII：Three-compon

8、entreactioncatalyze