Radiolabeling of Aryl Boronic Ester Derivatives for Cu Catalyzed At-211 Astatination of Biomolecules

dc.contributor.authorLinsten, Emma
dc.contributor.departmentChalmers tekniska högskola / Institutionen för kemi och kemitekniksv
dc.contributor.examinerVollmer Retegan, Teodora
dc.contributor.supervisorAneheim, Emma
dc.date.accessioned2020-06-30T11:58:48Z
dc.date.available2020-06-30T11:58:48Z
dc.date.issued2020sv
dc.date.submitted2020
dc.description.abstractTargeted alpha therapy is an area of research for treatment of spread microscopic cancer. Among theradioactivenuclidesthatemitalpha-radiationandareeligibleforuseintargetedalphatherapy, the astatine isotope 211At has been seen as a promising candidate. A common method of attaching the astatine to a targeting biomolecule has used a type of alkyltin reagent as a linking molecule. Since alkyltins are very toxic their use is not preferred. In 2016, an alternative copper catalyzed methodusinganarylboronicacidderivativeasalinkingmoleculewaspresented. In2018,thesame methodwasappliedonarylboronicesterderivativesaswell. Inthesepreviousstudiesofthecopper catalyzedmethod,theradioactivenuclidewasattachedtothelinkingmoleculewhichcouldthenbe conjugated to a targeting biomolecule. In order to minimize radiation dose, the preferred method of attachment would be to conjugate the linking molecule to a targeting biomolecule first and then attachtheradioactivenuclide. Thepossibilityofusingthecoppercatalyzedmethodforattachment toanalreadyconjugatedbiomoleculewasinvestigatedbyexaminingreactionconditionswhichcould make a transition from a reaction in organic solution to a reaction in aqueous solution possible. As a reaction in aqueous solution proved possible with good yields, the reaction was investigated for attachingthenuclidetoaconjugatedbiomolecule. Afteroptimizingthereactionconditions,ayield of 57.8% was achieved which indicated that the copper catalyzed method could be used to attach a radionuclidetoaconjugatedbiomolecule. Byfurtheroptimizingthereaction,itseemsplausiblethat thecoppercatalyzedmethodcanreplacethealkyltinrequiringmethodsv
dc.identifier.coursecodeKBTX12sv
dc.identifier.urihttps://hdl.handle.net/20.500.12380/301104
dc.language.isoengsv
dc.setspec.uppsokPhysicsChemistryMaths
dc.subjectIodinationsv
dc.subjectastatinationsv
dc.subjectradiopharmaceuticalssv
dc.subjecttargeted alpha therapysv
dc.subjectarylboronicester derivativesv
dc.titleRadiolabeling of Aryl Boronic Ester Derivatives for Cu Catalyzed At-211 Astatination of Biomoleculessv
dc.type.degreeExamensarbete för masterexamensv
dc.type.uppsokH
local.programmeMaterials chemistry (MPMCN), MSc
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