PRODUCTION OF RADIOIODINATED 1-β-D-ARABINOFURANOSYL)-5(E)-(2-IODOVINYL)URACIL, AND USES THEREOF, AND RELATED ANALOGUES INCORPORATING ALTERNATIVE HALOGEN RADIONUCLIDES, THE GENERAL RADIOHALOGENATION PRECURSORS, 1-(2,3,5-TRI-O-ACETYL-β-D-ARABINOFURANOSYL)-5(Z and E)-(2-TRIMETHYLSILYLVINYL)URACIL, PROCESSES FOR RADIOHA

摘要

Radioactive antiviral compounds, with 1-(β-D-arabinofuranosyl)-5(E)-(2-[*I]-iodovinyl)uracil, hereinafter referred to as '[*I]-IVaraU', as the prototype compound for the class of compounds designated as 1-β-D-arabinofuranosyl)-5(E)-(2-[*X]-halogenovinyl)uracil, hereinafter referred to as '[*X]-XVaraU', and novel precursors thereof, 1-(2,3,5-tri-O-acetyl-β-D-arabinofuranosyl)-5(Z and E)-(2-trimethylsilylvinyl)uracil, hereinafter referred to as 'TMSVaraU', and processes for the preparation thereof, and uses thereof, wherein '*I' stands for a radionuclide of iodine, and '*X' stands for any other appropriate halogen radionuclide. Inclusion of the appropriate gamma or positron emitting iodine, or other appropriate halogen radionuclide, into the structure of [*I]-IVaraU, makes this agent useful as a diagnostic tool for detection of herpes virus infections in vitro and in vivo. Inclusion of the appropriate alpha- and/or beta- and/or gamma- emitting, and/or Auger electron decay-associated, (specifically-nuclear-toxic) isotopes of iodine, or other appropriate halogen radionuclides, into the structure of this agent makes the agent useful as a unique radiotherapeutic tool for herpes virus infections by precise targeting of the lethal effects of alpha and/or beta radiation and/or Auger electron decay effects to the site of viral infection.