Bioorganic & Medicinal Chemistry Letters 1998-06-02

Rapid synthesis of a 5'-fluorinated oligodeoxy-nucleotide: a model antisense probe for use in imaging with positron emission tomography (PET).

D Pan, S S Gambhir, T Toyokuni, M R Iyer, N Acharya, M E Phelps, J R Barrio

Index: Bioorg. Med. Chem. Lett. 8(11) , 1317-20, (1998)

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Abstract

5'-Deoxy-5'-fluoro-O4-methylthymidine was synthesized by the reaction of the corresponding 5'-O-tosylate with KF in the presence of Kryptofix [222] and coupled to a 5'-phosphoramidite-activated CPG-bound oligodeoxynucleotide. The sequence of reactions and purifications were accomplished within 4 h, a necessary condition of the development of radiofluorinated antisense oligodeoxynucleotide probe for use with PET.