以7-氮雜吲哚為內(nèi)在導(dǎo)向基團(tuán)的N-芳基C-H官能化研究進(jìn)展（英文）

以7-氮雜吲哚為內(nèi)在導(dǎo)向基團(tuán)的N-芳基C—H官能化研究進(jìn)展（英文）Title:RecentAdvancesinN-ArylationofC-HBondsusing7-AzaindoleasanInternalDirectingGroupAbstract:TheN-arylationofC-Hbondsusing7-azaindoleasaninternaldirectinggrouphasemergedasapowerfulstrategyfortheconstructionofstructurallydiversenitrogen-containingcompounds.Thisreviewhighlightstherecentadvancesinthisfield,focusingonthedevelopmentofefficientandselectivemethodologiesfortheinstallationofarylgroupsontoC-Hbondsusing7-azaindoleasthedirectinggroup.Varioussyntheticstrategies,includingtransition-metal-catalyzedmethodologiesandmetal-freeapproaches,arediscussedalongwiththeirmeritsandlimitations.Additionally,thescopeandlimitationsofthesemethods,aswellastheirpotentialapplicationsinorganicsynthesisanddrugdiscovery,arealsoexplored.Keywords:7-azaindole,N-arylation,C-Hfunctionalization,directinggroup,syntheticmethodologies.1.IntroductionThedevelopmentofefficientandselectivemethodsforthefunctionalizationofC-Hbondsisanongoingareaofresearchinorganicsynthesis.AmongvariousdirectinggroupsemployedforC-Hfunctionalization,7-azaindolehasgainedsignificantattentionduetoitsabilitytoserveasaninternaldirectinggroupforN-arylationreactions.Thepresenceofbothanitrogenandanelectron-richindolemoietyin7-azaindolemakesitanidealcandidatefordirectingtheregioselectiveC-Hactivation.ThisreviewaimstoprovideanoverviewofrecentadvancesintheN-arylationofC-Hbondsusing7-azaindoleasthedirectinggroup.2.Transition-Metal-CatalyzedN-ArylationTransition-metal-catalyzedN-arylationreactionshavebeenextensivelyexploredforthefunctionalizationofC-Hbondsusing7-azaindoleasadirectinggroup.Varioustransitionmetals,suchaspalladium,copper,andnickel,havebeenemployedtopromoteC-Hactivationandsubsequentarylation.Differenttypesofarylatingagents,includingarylhalides,arylboronicacids,andaryltriflates,havebeenusedinthesereactions.Thedevelopmentofligandsandreactionconditionshasplayedacrucialroleinachievinghighselectivityandefficiencyinthesetransformations.Severalexamplesoftransition-metal-catalyzedN-arylationusing7-azaindoleasthedirectinggroupwillbediscussed.3.Metal-FreeN-ArylationInrecentyears,metal-freemethodologiesfortheN-arylationofC-Hbondsusing7-azaindoleasadirectinggrouphavealsoemergedaspromisingalternatives.Theseapproachesofferadvantagessuchasmildreactionconditions,lowtoxicity,andoperationalsimplicity.Differenttypesofarylatingagents,includingdiaryliodoniumsalts,diazoniumsalts,andarylboronicacids,havebeenusedinmetal-freeN-arylationreactions.Thedevelopmentofcatalystsandreactionconditionshasbeencrucialforachievinghighregioselectivityandfunctional-groupcompatibility.Variousexamplesofmetal-freeN-arylationusing7-azaindoleasthedirectinggroupwillbediscussed.4.ScopeandLimitationsThescopeandlimitationsofN-arylationusing7-azaindoleasadirectinggroupwillbediscussedinthissection.Factorssuchasthepositionoftheazaindoledirectinggroup,thenatureofthearylatingagent,andthefunctionalgroupspresentinthesubstratemayinfluencetheefficiencyandselectivityofthereaction.Additionally,theregioselectivityoftheC-Hactivationandthecompatibilityofthereactionconditionswithotherfunctionalgroupswillalsobeexplored.5.ApplicationsinOrganicSynthesisandDrugDiscoveryThesyntheticutilityoftheN-arylationofC-Hbondsusing7-azaindoleasadirectinggroupwillbehighlightedinthissection.TheabilitytoinstallarylgroupsontoC-Hbondsinaregioselectivemannerallowsfortherapidsynthesisofcomplexnitrogen-containingcompounds.Furthermore,theimportanceofthesecompoundsindrugdiscoverywillbediscussed,withseveralexamplesofbioactivemoleculessynthesizedusingthismethodology.6.ConclusionTheN-arylationofC-Hbondsusing7-azaindoleasaninternaldirectinggrouphasemergedasavaluablestrategyfortheconstructionofnitrogen-containingcompounds.Transition-metal-catalyzedandmetal-freemethodologieshavebeendevelopedtoachievehighefficiencyandselectivityinthesereactions.Thisreviewhasprovidedanoverviewofrecentadvancesinthisfield,highlightingthepotentialapplicati