Synthesis of 5-radiohalo-2'-deoxyuridine

Details Synthesis of 5-radiohalo-2'-deoxyuridine Synthesis of 5-radiohalo-2'-deoxyuridine

1993-12-30

1995-11-21

Robinson, Douglas W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

514 50, 536 553, C07H, C07H 1910, A61K 3170

Patent

active

054688531

ABSTRACT:
Method of synthesizing 5-radio-halogenated-2'-deoxyuridine from 5-trimethylstannyl-2'-deoxyuridine is described. The method consists of the steps of mixing 5-trimethylstannyl-2'-deoxyuridine with an aqueous solution consisting of a radiohalide and NaOH to form a first mixture, adding H.sub.2 O.sub.2 /CH.sub.3 COOH to the first mixture to form a second mixture, sonicating the second mixture, evaporating the solvent from the second mixture to form a residue, reconstituting the residue, filtering the residue; and then purifying the filtered residue such that at least one of a radiohalogenated nucleoside and nucleotide is obtained. A kit consisting of the components required for the above synthesis is also described.

REFERENCES:
patent: 4851520 (1989-07-01), Kassis et al.
Wigerinck et al. J. Med. Chem. 36:538-543, 1993.
Baranowska-Kortylewicz, et al., Radioiodomercuration: a Simple Synthesis of 5-[.sup.123/125/127 I]Iodo-2'-Deoxyuridine, Appl. Radiat. Isot. vol. 39, No. 4, pp. 335-341, 1988.
Bakker, et al., The Electrophilic Iodination with .sup.131 I of N.sub.1 -substituted Uracils Using Chloramine-T as Oxidant, Int. J. Radiat. Appl. Radiat. Isot. vol. 32, pp. 176-178, 1981.
Keough, et al., An Improved Method for Synthesis and Purification of .sup.125 I or .sup.131 I Labeled Carrier-Free 5-Iodo-2'-Deoxyuridine, J. of Labelled Comp. and Radipharmaceuticals, vol. XIV, No. 1, pp. 83-90, 1978.

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