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213Vol.21No.319998JournalofNuclearandRadiochemistryAug.19993B:1998205220:1999202215:,28,,()3(,100871)6222,3,422O22A2D2(6222,3,422O22A2D2),(IR)(1HNMR)(H22)Q503O629113(boronneutroncapturetherapy,BNCT),BNCT,,BNCT,,(PET)18F2FDGBNCTBNCT[B12H12]2-,,,,[B12H12]2-,[1][B12H11SH]2-[2][B12H11OH]2-[3],[B12H11SH]2-,[4],[58],[4][B12H11SH]2-,[B12H11OH]2-,,BNCT1111683,PerkinElmer;Dmx2300,Bruker;1106,CarloErbo;721,(Na2B12H12),;112(1822g)Hepatoma22A(H22)H22710610d,(015018)cm(0.50.8)cm,80500mg,100200mg,35LgB,,3015123h,,1,12[9]5,1136--2,3,4--O--A-D-6226222,3,422O22A2D2(C13H19O8I)[10],2(Cs2B12H11OH)[11],12IR1HNMR,200mgC13H19O8I((1))200mgCs2B12H11OH((2))136mgKOH20mL(DMSO),8548h,,,10mL,,,,216mg[N(C4H9)4]Br,,3,30111mg((3)),6715%3IR(Röcm-1):2937,2847(BH),1060(BB),1736(RCOOR)1HNMR(D):2.072.02(CH3COO),4.904.83(CH2),3.773.48(OCH3),2.041.87(BH)()(%):C,56164(57114);H,10181(10181);N,2138(2196)114(6--2,3,4--O--A-D-)Cs2B12H11SH[12][8],013gCs2B12H11SH01075gC13H19O8I30mL,48h,,,,CsB12H11S(C13H19O8)2[(4)]IR(Röcm-1):2837(BH),1075(BB),1746(RCOOR)1HNMR(D):21031194(CH3COO),41974195(CH2),31733142(OCH3),210112(BH)()(%):C,33162(34122);H,5121(5142);S,3107(3151)Cs2B12H11SH(4)42122O2((3),,)2S2((4))(Lg)4512116226222,3,422O22A2D2Fig.1Schemeforsynthesisof62iodo262deoxo22,3,42tri2O2acetyl2A2D2methylglucoside22Fig.2Schemeforsynthesisofcesiumhydroxyundecahydro2closo2dodecaborate(22)5513:36222,3,422O22A2D2Fig.3Schemeforsynthesisoftetrabutylammonium62deoxo22,3,42tri2O2acetyl2A2D2methyl2glucoside2oxo2undecahydro2closo2dodecaborate(22)4(6222,3,422O22A2D2)Fig.4Schemeforsynthesisofcesiumbis(62deoxy22,3,42tri2O2acetyl2A2D2methylglucoside)sulfido2undecahydro2closo2dodecaborate(12)12,:(1),;(2)1h,,;(3),;(4)1h,R(TöB)11821187,BNCTBSH()(BSHR(TöB)=0.6114[13]),B,1g10LgB,BSH85170mg,24,,(3):,,,;(4):,,,651211B12H11OA-DH22Table1BiodistributionofB12H11O-containingA-DmethylglucosideinH22tumor-bearingmiceLg(tissue)015h110h210h310hm(B)m(B)sm(B)m(B)sm(B)m(B)sm(B)m(B)s(liver)(tumor)(blood)(lung)12161101848167713161572105313521922136216621792165215311802131512641763185416531039122132167015821420144413101582516023175231952310820167812513180101591219991137102615361035131512813154121781210114127101352314110111021561030173121611019162171051712718164131473196315741123136319231533162315821913101613651736154613751441712112317901353133013461090136121571012691501118591272118119721262196212711871135112311171174419741654107414731811017114213301431148013141390138(note):m(B)B(Lg),(m(B)inthisandsubsequenttablerepresentsBcontent(Lg)in1gtissue)2B12H11SA-D-H22Table2BiodistributionofB12H11S-containingA-D-methylglucosideinH22tumor-bearingmiceLg(tissue)015h110h210h310hm(B)m(B)sm(B)m(B)sm(B)m(B)sm(B)m(B)s(liver)(tumor)(blood)(lung)1217311174101569168719931522196317431924185216421972163116221125176412341894138312810151183180016921400158415101692316721189191672015517131121631018712153101431010961345161510751324108513161737165517651212016114111311151280155611301981814316195151731611514126414751645149415631823112218621972165117941035145610341284176161311541800161216801204191019512174121311018611154912821062146219421793122116511821152114701895115416831793168312111141142169013911470116411001717513:BSH(1)(4),[4]S2[C6H11O5SB12H11]2-,BSH(),(3),,R2OH+S2O2[B12H11OH]2-BSH,BOBS40pm[6],2O2[4]S2[C6H11O5SB12H11]2-,1hR(TöB)217()819(),,[4,8]HPLCS2,,:(4)BSH,BSH,BSH,3,10B,:,1GmelinHandbuchderanorganischenChemie,Band54,Borverbindungen,Teil20.Berlin2Heidelberg2NewYork:Springer2Verlag.1979.2162GabelD,MollerD,Harfst,etal.SynthesisofS2alkylandS2acylDerivativesofMercaptounde2cahydrododecaborate,aPossibleBoronCarrierforNeutronCaptureTherapy.InorgChem,1993,32:22763PeymannT,LorkE,GabelD.Hydroxoundecahydro2closo2dodecaborate(22)asaNucleophile,PreparationandStructuralCharacterizationofO2AlkylandO2AcylDerivativesofHydroundecahydro2closo2dodecabo2rate(22).InorgChem,1996,35:13554PeymannT,PresseD,GabelD.SynthesisofS2glycosidesofMercaptoundecahydro2closo2dodecaborate(22)In:LarssonB,CrawfordJ,WeinreichR.eds.AdvancesinNeutronCaptureTherapy,(Ê).ChemistryandBiology.Amsterdam2Lausanne2NewYork2Oxford2Shannon2Singapore2Tokyo:Elsevier.1997.355MaurerJL,BerichierF,SerinoAJ,etal.GlycosylcarboraneDerivativesandtheDeterminationoftheAbso2luteConfigurationofaDiastereomericTriolFromX2rayDiffraction.JOrgChem,1990,55,8386MaurerJL,SerinoAJ,HawthorneMF.HydrophilicallyAugmentedGlycosylCarboranylDerivativesforIncorporationinAntibodyCojugationReagents.Organometallics,1988,7:25197TjarkW,AnisuzzanmanAKM,SolowayAH.Synthesisof1,32Di2acetyl252O2benzoyl222(O2carboran212ylmethyl)2ribofuranose:aGeneralPrecusorforthePreparationofCarborane2containingNucleosidesforBoronNeutronCaptureTherapy.NucleosidesNucleotides,1992,11:17658GabelD,HarfastS,MollerD,etal.PreparationandPurificationofB12H11S2containingCompoundsforBoronNeutronCaptureTherapy.In:KabalkaGWed.CurrentTopicintheChemistryofBoron.Cam285121bridge,UK:TheRoyalSocietyofChemistry.1996,1619KaczmarzykA,MesserJR,PeirceCE.RapidMethodforDeterminationofBoroninBiologicalMaterials.AnalChem,1997,43(2):27110RaymondAL,SchroederE.Synth