AI Article Synopsis
- Organotin intermediates were utilized to synthesize IVaraU through a reaction involving a specific uracil compound and a stannyl ethene in the presence of a palladium catalyst.
- The synthesized precursor reacted with radioiodine isotopes ([123I] or [125I]) in methanol to yield no-carrier-added ([123I]IVaraU) with radiolabeling efficiency up to 97%, and was purified using reversed phase HPLC.
- An alternative radioiodination method using BrVara U and a cuprous ion catalyst also achieved high yields (up to 93%) for no-carrier-added [123,125I]IVaraU under exchange conditions.
Article Abstract
Organotin intermediates for IVaraU synthesis were obtained following the reaction of 1-(2',3',5'-tri-O-toluyl-beta-D-arabinofuranosyl-5-iodouracil with (E)-1,2-bis(tri-(n-butyl) stannyl)ethene in the presence of catalytic (Ph3P)2PdCl2. A direct precursor for IVaraU, (E)-5-[2-tri-n-butylstannylvinyl]-arabinosyluridine, reacted with [123I]NaI (10 mCi) or alternatively [125I]NaI in the presence of methanol and chloramine T providing no-carrier-added (NCA) [123I]IVaraU in a radiolabeling yield up to 97%; the product was recovered following reversed phase HPLC. Unlabeled IVaraU was prepared in five steps from arabinosyluridine via an organotin intermediate with an overall yield of 22%. An exchange radioiodination was also identified, based on accessible BrVara U in the presence of water and a cuprous ion catalyst. [123I]NaI (up to 40 mCi) or alternatively [125I]NaI reacted under exchange conditions to give no-carrier-added [123,125I]IVaraU in a radiolabeling yield of 93%; the product was recovered following reversed phase HPLC.
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| http://dx.doi.org/10.1016/0969-8043(94)90131-7 | DOI Listing |
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