Synthesis and Radioiodination of 7-(3´-Ammoniopropyl)-7,8-dicarba-nido-undecaborate(-1), (ANC)

Derivatives of nido-carborate have potential use in tumour targeting as hydrophilic boron-rich compounds for boron neutron capture therapy (BNCT) and as pendant groups for attachment of radiohalogens to tumour-seeking molecules. For this purpose, functionalized derivatives of nido-carborates that can be conjugated to biomolecules should be synthesized and evaluated. In this study, racemic 1, 7-(3′-ammoniopropyl)-7,8-dicarba-nido-undecaborate(-1) (acronym ANC) was obtained by degradation of the corresponding aminopropyl-o-carborane, which was synthesized in three steps from 1-tert-butyldimethylsilyl-2-(3-bromopropyl)-o-carborane, with sodium hydroxide in absolute ethanol. The racemate 1 was radioiodinated (125I) using the Chloramine-T method. Radio-TLC results showed that radiolabelling with 125I was achieved in a yield greater than 95%.

Malmquist, JonasUppsala universitet,Kemiska institutionen (author)
Lundquist, HansUppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi (author)
Tolmachev, VladimirUppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi(Swepub:uu)vladtolm (author)
Sjöberg, StefanUppsala universitet,Kemiska institutionen(Swepub:uu)stefsjob (author)
Uppsala universitetKemiska institutionen (creator_code:org_t)

In:Journal of labelled compounds & radiopharmaceuticals: Wiley47:9, s. 557-5690362-48031099-1344

By the author/editor: Ghirmai, Senait; Malmquist, Jonas; Lundquist, Hans; Tolmachev, Vladi ...; Sjöberg, Stefan

About the subject

NATURAL SCIENCES: NATURAL SCIENCES; and Chemical Science ...; and Organic Chemistr ...

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