Radiolabeling of Aryl Boronic Ester Derivatives for Cu Catalyzed At-211 Astatination of Biomolecules
dc.contributor.author | Linsten, Emma | |
dc.contributor.department | Chalmers tekniska högskola / Institutionen för kemi och kemiteknik | sv |
dc.contributor.examiner | Vollmer Retegan, Teodora | |
dc.contributor.supervisor | Aneheim, Emma | |
dc.date.accessioned | 2020-06-30T11:58:48Z | |
dc.date.available | 2020-06-30T11:58:48Z | |
dc.date.issued | 2020 | sv |
dc.date.submitted | 2020 | |
dc.description.abstract | Targeted 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 thecoppercatalyzedmethodcanreplacethealkyltinrequiringmethod | sv |
dc.identifier.coursecode | KBTX12 | sv |
dc.identifier.uri | https://hdl.handle.net/20.500.12380/301104 | |
dc.language.iso | eng | sv |
dc.setspec.uppsok | PhysicsChemistryMaths | |
dc.subject | Iodination | sv |
dc.subject | astatination | sv |
dc.subject | radiopharmaceuticals | sv |
dc.subject | targeted alpha therapy | sv |
dc.subject | arylboronicester derivative | sv |
dc.title | Radiolabeling of Aryl Boronic Ester Derivatives for Cu Catalyzed At-211 Astatination of Biomolecules | sv |
dc.type.degree | Examensarbete för masterexamen | sv |
dc.type.uppsok | H | |
local.programme | Materials chemistry (MPMCN), MSc |