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1、Aone-potsynthesisofisoindolin-1-iminederivativesAone-potsynthesisofisoindolin-1-iminederivativesKhangvanPhama,ZhongguoZhanga,SidaShena,LeiMaa,*,LihongHua,b,*aShanghaiKeyLaboratoryofNewDrugDesign,SchoolofPharmacy,EastChinaUniversityofScienceandTechnol
2、ogy,130MeilongRoad,Shanghai200237,PRChinabShanghaiResearchCenterforModernizationofTraditionalChineseMedicine,ShanghaiInstituteofMateriaMedica,ChineseAcademyofSciences,Shanghai201203,PRChinaarticleinfoArticlehistory:Received10September2013Receivedinre
3、visedform16October2013Accepted21October2013Availableonline30October2013Keywords:2-Cyanobenzaldehyde4-HydroxycoumarinIsoindolin-1-imine4-Hydroxyquinolin-2(1H)-oneOne-potreactionabstractAone-potprocedurewasdevelopedforthesynthesisofisoindolin-1-iminede
4、rivativesbyasimplethree-componentcondensationof2-cyanobenzaldhyde,ammoniumacetate,and4-hyroxycoumarinde-rivativesor1,3-dicarbonylcompoundsor4-hydroxyquinolin-2(1H)-oneinethanolunderrefluxfor20e60minwithexcellentyields.Theadvantagesofthisprocedureareo
5、perationalsimplicity,excellentyields,andshortreactivetime,withoutcatalyst,easyworkup,andgreenenvironmentalimpact.?2013ElsevierLtd.Allrightsreserved.1.IntroductionIsoindoleanditsderivativesareoneofthemostimportantclassesofN-heterocyclicbiologicalactiv
6、ecompounds.1Theyhavebeenreceivedconsiderableattentionfromsyntheticpharmacistsandchemistsduetotheirpotenttherapeuticandpharmacologicalactivities.1,2Isoindolin-1-imineseriesareanimportantclassofisoindoles,andhaveexhibitedtypicalpharmacologicalactivitie
7、s,includingasNR2B-selectiveNMDAreceptorantagonists,2cthethrombinreceptor(PAR-1)inhibitors,2c,dandantiproliferativeeffect.2Sincethefirstmulti-componentreaction(MCR)wasaccom-plishedin1850byStrecker,4aMCRshavebeenespeciallyimportanttotheorganicsynthesis
8、duetooperationalsimplicity,highpro-ductivity,shortreactiontime,andhighyieldwithoutisolatingtheintermediatesfromsimpleandpopularstartingmaterials.4Uptodate,manywell-knownMCRs,suchasalkynetrimerization,4bKabachnikeFieldsreaction,4cBiginellireaction,4dA
